Mohammad, T.’s team published research in Journal of Labelled Compounds and Radiopharmaceuticals in 1986-07-31 | CAS: 27483-92-7

Journal of Labelled Compounds and Radiopharmaceuticals published new progress about thioridazine deuterated. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Recommanded Product: 2-(Chloromethyl)-1-methylpiperidine hydrochloride.

Mohammad, T. published the artcileSynthesis of deuterium-labeled thioridazine, Recommanded Product: 2-(Chloromethyl)-1-methylpiperidine hydrochloride, the main research area is thioridazine deuterated.

A 7-step synthetic route to (±)-thioridazine I (R = R1 = H) was developed starting from racemic Et 1-methyl-2-piperidinecarboxylate. LiAlD4 reduction of the starting and homologous esters allowed the incorporation of D in the 1- and/or 2-position(s) of the Et side chain of thioridazine. The isotopic purity of I (R = R1 = D; R = H, R1 = D; R = D, R1 = H) was >99%.

Journal of Labelled Compounds and Radiopharmaceuticals published new progress about thioridazine deuterated. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Recommanded Product: 2-(Chloromethyl)-1-methylpiperidine hydrochloride.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Taguchi, Tanezo’s team published research in Chem. Pharm. Bull. (Tokyo) in 1965 | CAS: 27483-92-7

Chem. Pharm. Bull. (Tokyo) published new progress about Alcohols. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Quality Control of 27483-92-7.

Taguchi, Tanezo published the artcileHeteroalicyclic aminoalkanols. II. Reactions of DL-2-piperidylmethanol involving the formation of DL-1-azabicyclo[4.1.0]heptane, Quality Control of 27483-92-7, the main research area is .

2-Piperidylmethanol (I) (5 g.) in 5 cc. Et2O treated simultaneously with stirring at 0° with 6 g. BzCl in 20 cc. Et2O and 20 cc. aqueous NaOH and stirred 1 h. at room temperature yielded 7.2 g. 1-Bz derivative (II) of I, granules, m. 94-5° (Et2O). II (0.5 g.) in 20 cc. 2% aqueous HCl gave 0.53 g. benzoate (III) of I.HCl, rods, m. 243-4° (MeOH-EtOH). II with 2% HBr gave similarly 91% I.HBr, needles, m. 233-4° (decomposition) (EtOH). III.HCl (0.2 g.) stirred 0.5 h. with 10 cc. 5% aqueous NaOH yielded 0.15 g. II, granules, m. 74° (Et2O). I (1.15 g.) in 10 cc. Et2O treated dropwise with 9 cc. aqueous NaOH and then with 3 g. BzCl and stirred 3 h. yielded 2.8 g. 1-benzoyl-2-piperidylmethanol benzoate (IV), granules, m. 65-7° (Et2O-ligroine). II (0.5 g.) in 5 cc. C6H6 and 5 cc. 10% aqueous NaOH treated dropwise with stirring with 0.4 g. BzCl gave 0.66 g. IV, m. 65°. I ( 1 g.), 0.88 cc. BzH, and 10 cc. C6H6 refluxed 1 h. with 1 cc. AcOH with the azeotropic removal of H2O gave 1.3 g. V, b8 134-6°. V (0.5 g.) in 2 cc. CHCl3 treated dropwise with cooling and stirring with 0.4 g. Br in 2 cc. CHCl3 and then stirred with 2 cc. 10% aqueous NaOH gave 0.67 g. III.HBr, needles, m. 233° (EtOH). 2-ClCH2 analog (VI) (4 g.) of I.HCl and 2 g. CS(NH2)2 in 12 cc. EtOH refluxed 10 h. gave 2.5 g. 2-(2-pyridylmethyl)-2-thiopseudourea-2HCl (VIa.2HCl), needles, m. 182-4° (EtOH), and 0.8 g. VII.HCl, rods, m. 186-8° (BuOH). VIa.2HCl (0.2 g.) in 2 cc. BuOH refluxed 1 h. yielded 0.18 g. VII.HCl, needles, m. 186-8° (BuOH). VIa.2HCl (50 mg.) in 2 cc. EtOH treated successively with 0.57 cc. 2% alc. KOH, 41 mg. 2,4-(O2N)2C6H3Cl in 2 cc. EtOH, and 1.14 cc. 2% alc. KOH yielded 25 mg. 1-(2,4-dinitrophenylamidino)-2-(2,4-dinitrophenylthiomethyl)piper-idine, brownish yellow granules, m. 185-7° (decomposition). 1-Methyl-2-piperidylmethanol (VIII) (3 g.) in 30 cc. dry Et2O and then 1.8 cc. CS2 added dropwise with cooling and stirring to 0.46 g. powd. Na in 25 cc. dry Et2O, treated with 1.24 cc. MeI in 5 cc. dry Et2O, and worked up gave 3.1 g. Me 1-methyl-2-piperidylmethyl xanthate (IX), yellow oil; picrate, yellow needles, m. 124-6° (EtOH); IX.HCl m. 134-5° (EtOH-Et2O). The alk. hydrolysis of IX yielded VIII. VIII (4 g.) heated 0.5 h. at 130° yielded 3.5 g. S-(1-methyl-2-piperidylmethyl) S’-Me dithiolcarbonate (X), light yellow oil, b1 119-20°; picrate m. 164-5° (EtOH). VIII (7 g.) in 20 cc. dry CHCl3 refluxed 3 h. with 6 cc. SOCl2 gave 7.1 g. 2-ClCH2 analog (XI) of VIII.HCl, needles, m. 159-61° (Me2CO). XI.HCl (3 g.) and 1.23 g. CS(NH2)2 in 10 cc. EtOH refluxed 4 h. yielded 2.8 g. 2-(1-methyl-2-piperidylmethyl)-2-thiopseudourea-2HCl (XII.2HCl), needles, m. 192-3° (BuOH). XII.2HCl (0.7 g.) heated 1 h. on the water bath with 5 cc. 2N NaOH and treated with a stream of air gave 0.68 g. bis(1-methyl-2-piperidylmethyl) disulfide (XIII); dipicrate m. 153-5° (MeOH). X (1 g.) and 40 cc. 5% alc. NaOH heated I hr. on the water bath, treated dropwise with 10% alc. HCl (EtSH evolved), and the crude product treated in aqueous K2CO3 with air overnight yielded 0.8 g. XIII picrate, m. 151-4° (MeOH). VIII.MeI (8 g.) and Ag2O from 12 g. AgNO3 and 20 cc. 10N NaOH stirred 5 h., filtered, and evaporated, and the residue heated 3 h. at 100° in vacuo under N gave 1 g. VIII and 1.1 g. Me2N(CH2)5CHO, b3 168-70°; picrate m. 146-8° (H2O). I (6 g.) added with cooling to 5 cc. concentrated H2SO4 and heated gradually to 240° yielded 7.4 g. 2-HO3SOCH2 analog (XIV) of I, rods, m. 262-3° (decomposition) (MeOH). XIV (6 g.) in 40 cc. H2O and 100 cc. 10% aqueous NaOH distilled and the distillate treated with solid KOH gave 0.2 g. XV, b80 65°, which polymerized completely within several hrs., even under N; XV picrate m. 151-2° (Et2O-AcOEt). XV (0.1 g.) in Et2O stirred 1 h. and treated with K2CO3, and the basic product treated with picric acid gave the picrate of I, m. 115° (EtOH-Et2O). XV (0.1 g.) in Et2O treated with dry HCl and kept overnight gave VI.HCl, m. 187-8°. XV (0.1 g.) in Et2O treated overnight with 0.1 g. MeBr in Et2O gave 0.16 g. 2-bromomethyl-1,1-dimethylpiperidinium bromide (XVI), granules, m. 230° (EtOH). XV (0.14 g.), 0.1 g. CS(NH2)2, 1.32 cc. N HCl, and 2 cc. H2O stirred a few min., treated with an addnl. 1.32 cc. N HCl, and stirred 1 h., and the crude product refluxed 1 h. in BuOH gave VII isolated as the picrate, m. 1523° (H2O). I (3 g.) in 30 cc. 48% aqueous HBr refluxed 10 h. yielded 4.1 g. 2-bromomethylpiperidine-HBr (XVII.HBr), needles, m. 188-90° (EtOH). XVII.HBr (0.5 g.) in 10 cc. Et2O treated overnight with 20 cc. 10% MeBr-Et2O gave 0.57 g. XVI, granules, m. 233-4° (decomposition) (EtOH).

Chem. Pharm. Bull. (Tokyo) published new progress about Alcohols. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Quality Control of 27483-92-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Kasuga, Seiki’s team published research in Chemical & Pharmaceutical Bulletin in 1965 | CAS: 27483-92-7

Chemical & Pharmaceutical Bulletin published new progress about Alcohols. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Computed Properties of 27483-92-7.

Kasuga, Seiki published the artcileHeteroalicyclic aminoalkanols. I. Syntheses of DL-2-piperidylmethanol and meso-cis-2,6-bis(hydroxymethyl)piperidine and reactions of intermediates, Computed Properties of 27483-92-7, the main research area is ALCOHOLS; CHEMISTRY, PHARMACEUTICAL; EXPERIMENTAL LAB STUDY; PIPERIDINES; PYRIDINES.

2-Acetoxymethyl-6-methyl- pyridine 1-oxide (I) (20 g.) in 100 cc. 48% aqueous HBr refluxed 4 h. yielded 27.1 g. 2-BrCH2 analog (II) of I.HBr, colorless rods, m. 123-4° (Me2CO). 2,6-Bis(acetoxymethyl)pyridine 1-oxide (10 g.) yielded similarly 10.5 g. 2,6-bis(bromomethyl)pyridine 1-oxide (III), granules, m. 153-5° (MeOH). 2-Bromomethylpyridine 1-oxide-HBr (IV.HBr) (5 g.) treated with alkali, and the free IV heated 2.5 h. on the water bath with 1.2 cc. CS(NH2)2 in 100 cc. EtOH yielded 3.5 g. 2-(2-pyridylmethyl)-2-thiopseudourea N-oxide-HBr (V.HBr), rods, m. 184-5° (decomposition) (MeOH). II yielded similarly the 2-(6-methyl-2-pyridylmethyl) analog (VI) of V.HBr, rods, m. 191-2° (EtOH). III gave similarly 65% VII.2HBr, granules, m. 203-5° (decomposition). Na (0.34 g.) in 23 cc. absolute EtOH treated with dry H2S until alk. and then with IV in EtOH from 5 g. IV.HBr, and the resulting gummy product dissolved in 5 cc. 4N alc. HCl with warming, filtered from some bis-(1-oxo-2-pyridylmethyl) disulfide-2HCl (VIII.2HCl), and worked up yielded 2-pyridylmethanethiol 1-oxide-HCl (IX.HCl), rods, m. 114-15° (Me2CO). II gave similarly the 6-Me derivative (X) of IX.HCl, 21%, rods, m. 133-4° (EtOH), and some 6,6′-dimethyl derivative (XI) of VIII, m. 160-4°. VI (0.2 g.) in 0.6 cc. 2N NaOH heated 2 h. on the water bath under N, cooled, and acidified with alc. HCl yielded 0.02 g. X.2HCl, m. 132-3° (Et2O-EtOH). IV from 3 g. IV.HBr heated 2 h. on the water bath with 5 cc. H2O containing 1.34 g. Na2S.9H2O yielded 0.5 g. bis(1-oxo-2-pyridylmethyl) sulfide (XII), yellow rods, m. 1745° (decomposition); picrate m. 148° (EtOH). II gave similarly 35% 6,6′-dimethyl derivative of XII, light yellow rods, m. 121-2° (AcOEt); XI.2HCl, granules, m. 163-4° (EtOH). Na2S.9H2O (1.34 g.) and 0.23 g. S in 10 cc. H2O heated 2 h. on the water bath with IV from 3 g. IV.HBr, and the gummy product treated with 3 cc. 4N alc. HCl yielded 0.3 g. VlII.2HCl, rods, m. 1623° (decomposition) (MeOH); picrate m. 139-40° (EtOH). IX in EtOH aerated overnight gave VIII which was converted to the picrate, m. 135-9°. II treated with Na2S yielded 28% XI.2HCl, m. 192-3° (decomposition). X oxidized with air and treated with HCl gave 38.5% XI.2HCl, m. 192-3° (decomposition). IV from 2.8 g. IV.HBr stirred 2 h. with 40 cc. H2O containing 2.7 g. EtSNa yielded 0.5 g. oily, yellowish 2-ethylthiomethylpyridine 1-oxide (XIII), b6, 134-7°; picrolonate, m. 137° (EtOH). II gave similarly 39% yellow, oily 6-Me derivative of XIII, b3 143-6°; picrolonate m. 120.5-21° (EtOH). II (1 g.) refluxed 4 h. with 5 cc. Ac2O yielded 0.5 g. pink oil, b2 90-115° which refluxed 4 h. with 10 cc. 47% aqueous HBr gave 0.28 g. III.HBr, m. 208-10° (decomposition) (EtOH); the filtrate treated with 2,4-(O2N)2C6H3-NHNH2 in aqueous H3PO4 yielded 6-methylpyridine-2-carboxaldehyde 2,4-dinitrophenylhydrazone (XIV), m. 231-3° (decomposition). X in Ac2O refluxed 3 h. under N yielded 21% 6-methyl-2-pyridylmethanethiol acetate (XV), yellow oil, b5 112-14°; picrolonate m. 164-5° (decomposition) (EtOH). 2-Ethylthiomethyl-6-methylpyridine 1-oxide (3 g.) in 9 cc. Ac2O refluxed 4 h. yielded 3.4 g. 2-(acetoxy)(ethylthio)methyl-6-methylpyridine (XVI), pink oil, b5 143-4°; picrate m. 105-7° (aqueous EtOH). XVI (1 g.) and 20 cc. 20% aqueous HCl refluxed 10 h. under N (EtSH evolved) yielded 0.46 g. oil, b12 77-8°, which gave XIV, m. 230°. IV.HBr (1 g.) in 6 cc. 2N NaOH kept 1 h. at room temperature gave 0.41 g. bis-(1-oxo-2-pyridylmethyl) oxide H2O (XVII.H2O), needles, m. 128-9° (AcOEt); picrate m. 192-3° (EtOH). Bis(2-pyridylmethyl) oxide (XVIII) (0.2 g.), 2 cc. AcOH, and 0.4 cc. 30% H2O2 heated 12 h. at 70-80° gave 0.1 g. XVII.H2O, m. 127°. XVII.H2O (0.3 g.) in 15 cc. 48% HBr refluxed 7 h. yielded IV, isolated as the picrate, m. 129-30°. XVII.H2O (0.4 g.) in 30 cc. CHCl3 heated 1 h. on the water bath with 0.3 cc. PCl3 and basified with aqueous K2CO3 gave 0.23 g. oily XVIII, b4 146-8°; picrate m. 197-8° (decomposition) (EtOH). 2-Pyridylmethanol (XIX) (2 g.) in 10 cc. xylene treated with stirring and cooling with 5.4 g. concentrated H2SO4 and heated 5 h. at 160-70° with the azeotropic removal of H2O gave 1.6 g. unreacted XIX, b8 100-5°, and 0.22 g. XVIII, b3 145-8°. 2-Bromomethylpyridine-HBr (XX.HBr) (1 g.) stirred 5 h. with 10 cc. 2N NaOH gave 0.21 g. XIX, b4 74-80°, and 0.23 g. XVIII, b4 80-124°. II treated with PCl3 gave 82.3% bis(1-oxo-6-methyl-2-pyridylmethyl) oxide-0.5H2O (XXI.-0.5H2O), needles, m. 175-7° (MeOH); picrate m. 174-5° (EtOH). 6,6′-Dimethyl derivative (XXII) of XVIII in xylene refluxed with concentrated H2SO4 gave 78.5% XXI.0.5H2O. 6-Me derivative (XXIII) of XIX gave similarly unreacted XXIII and 33.8% XXII, b4 150-5°, which yielded a dipicrate, m. 210-12° (decomposition). The 6-Me derivative of XX stirred 5 h. with 2N NaOH yielded 63.2% XXII, m. 75-6° (H2O). XVII.H2O (5 g.) and 30 cc. Ac2O refluxed 4 h. yielded 1.4 g. picolinecarboxaldehyde diacetate, b3 118-23° [picrate m. 146-7° (EtOH)], and 2.15 g. 2-pyridylmethyl picolinate (XXIV), b0.05 155-7°, m. 52-3° (ligroine). Picolinic acid (1.6 g.) in 3 cc. C6H6 treated with cooling and stirring with 6 cc. concentrated H2SO4 and 1.1 g. XIX, and the mixture refluxed with the overhead removal of H2O-C6H6 azeotrope and the dropwise addition of C6H6 during 6 h., poured onto ice, and basified with aqueous K2CO3 yielded 0.5 g. unreacted XIX and 0.26 g. XXIV, m. 52-3° (ligroine). XIX (50 g.) in 50 cc. EtOH hydrogenated 7 h. with stirring at 80° and 200 atm. initial pressure over 50 cc. Raney Ni W-2 yielded 47.8 g. 2-piperidylmethanol, b13 108°; picrate m. 133-5° (EtOH). Di-Me meso-cis-2,6-piperidinedicarboxylate (1 g.), 0.5 g. LiAlH4, and 40 cc. Et2O refluxed 3 h. yielded 1.5 g. meso-cis-2,6-bis(hydroxymethyl)piperidine (XXV), plates, m. 130-1° (AcOEt). 2,6-Bis(hydroxymethyl)pyridine (4 g.) in 20 cc. EtOH hydrogenated over 10 cc. Raney Ni yielded 3.4 g. XXV. Di-Me 2,6-pyridinedicarboxylate (3.5 g.) in 35 cc. MeOH hydrogenated over 15 cc. Raney Ni gave 2.2 g. XXV, plates, m. 128-30°.

Chemical & Pharmaceutical Bulletin published new progress about Alcohols. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Computed Properties of 27483-92-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Anderson, Fiona M.’s team published research in Anti-Cancer Drug Design in 2000-04-30 | CAS: 27483-92-7

Anti-Cancer Drug Design published new progress about Alkylating agents. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, COA of Formula: C7H15Cl2N.

Anderson, Fiona M. published the artcileSynthesis of new homochiral bispyrrolidines as potential DNA cross-linking antitumor agents, COA of Formula: C7H15Cl2N, the main research area is structure activity antitumor bispyrrolidine DNA crosslinking.

We are seeking to develop more effective bifunctional alkylating agents as antitumor agents. We previously synthesized conformationally restricted nitrogen mustards containing one piperidine ring, then bispiperidine derivatives were designed and prepared with varying lengths of carbon chain between the two rings and structure-activity relationships in these systems were studied. A bispiperidine with the shortest bridge of two carbon atoms was the most reactive bifunctional alkylating agent. In order to extend this work and investigate the effects of a change in the size of the heterocyclic systems, new bispyrrolidine salts 17-23 with chloromethyl groups at the 2-positions and a bridge between the two nitrogen atoms of 2-8 carbon atoms were synthesized from L-proline so that only the LL-enantiomers were produced. The free bases were designed to be bifunctional alkylating agents via aziridinium ion formation with different distances between the two alkylating sites. All of the bispyrrolidines were efficient cross-linkers of naked DNA apart from those with three-carbon (18) and four-carbon (19) bridges, in contrast to the results with the bispiperidines. A piperazine derivative 24 with two potential alkylating sites was also shown to be an efficient cross-linker, as was an alicyclic compound 25 with six carbon atoms between the two alkylating sites. Compounds 26 and 30 with an extra carbon atom between the nitrogen and the leaving group were not cross-linkers, as expected if aziridinium ion formation is crucial for crosslinking ability. The preformed aziridine 27 with a further alkylating site was an efficient cross-linker. Compounds 28-29 with only one potential alkylating center were not cross-linkers of DNA. None of the compounds, however, produced significant cytotoxicity in human tumor cells in vitro.

Anti-Cancer Drug Design published new progress about Alkylating agents. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, COA of Formula: C7H15Cl2N.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Ngo, Huy X.’s team published research in ACS Infectious Diseases in 2018-06-08 | CAS: 27483-92-7

ACS Infectious Diseases published new progress about Antibacterial agent resistance. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Recommanded Product: 2-(Chloromethyl)-1-methylpiperidine hydrochloride.

Ngo, Huy X. published the artcilePotent 1,2,4-Triazino[5,6b]indole-3-thioether Inhibitors of the Kanamycin Resistance Enzyme Eis from Mycobacterium tuberculosis, Recommanded Product: 2-(Chloromethyl)-1-methylpiperidine hydrochloride, the main research area is triazinoindole thioether kanamycin resistance aminoglycoside acetyltransferase Eis Mycobacterium tuberculostatic; aminoglycoside resistance; antitubercular agent; combination therapy; high-throughput screen; structure-activity relationship (SAR).

A common cause of resistance to kanamycin (KAN) in tuberculosis is overexpression of the enhanced intracellular survival (Eis) protein. Eis is an acetyltransferase that multiacetylates KAN and other aminoglycosides, rendering them unable to bind the bacterial ribosome. By high-throughput screening, a series of substituted 1,2,4-triazino[5,6b]indole-3-thioether mols. were identified as effective Eis inhibitors. Herein, the authors purchased 17 and synthesized 22 new compounds, evaluated their potency, and characterized their steady-state kinetics. Four inhibitors were found not only to inhibit Eis in vitro, but also to act as adjuvants of KAN and partially restore KAN sensitivity in a Mycobacterium tuberculosis KAN-resistant strain in which Eis is upregulated. A crystal structure of Eis in complex with a potent inhibitor and Co-A shows that the inhibitors bind in the aminoglycoside binding site snugly inserted into a hydrophobic cavity. These inhibitors will undergo preclin. development as novel KAN adjuvant therapies to treat KAN-resistant tuberculosis.

ACS Infectious Diseases published new progress about Antibacterial agent resistance. 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Recommanded Product: 2-(Chloromethyl)-1-methylpiperidine hydrochloride.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Deng, Hongfeng’s team published research in Journal of Medicinal Chemistry in 2005-10-06 | CAS: 27483-92-7

Journal of Medicinal Chemistry published new progress about Labeled chemical compounds Role: DGN (Diagnostic Use), PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), USES (Uses), PREP (Preparation). 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Application In Synthesis of 27483-92-7.

Deng, Hongfeng published the artcilePotent Cannabinergic Indole Analogues as Radioiodinatable Brain Imaging Agents for the CB1 Cannabinoid Receptor, Application In Synthesis of 27483-92-7, the main research area is indole iodobenzoyl piperidinylmethyl radioiodinated preparation CB1 cannabinoid receptor agonist; iodine labeled indole brain imaging agent.

A series of novel aminoalkylindoles was synthesized in an effort to develop compounds that are potent agonists at the CB1 cannabinoid receptor and that are also easily labeled with radioisotopes of iodine for biochem. and imaging studies. 2-Iodophenyl-[1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl]methanone I (AM2233) had a very high affinity for the rat CB1 receptor, with most of the affinity residing with the (R)-enantiomer. Radioiodinated racemic I and its enantiomers were prepared by radioiododestannylation of the tributyltin analogs in high yields, radiochem. purities, and specific radioactivities. In a mouse hippocampal membrane preparation with [131I](R)-I as radioligand, racemic I exhibited a Ki value of 0.2 nM compared with 1.6 nM for WIN55212-2. In autoradiog. experiments with mouse brain sections, the distribution of radioiodinated I was consistent with that of brain CB1 receptors. Again, very little specific binding was seen with the (S)-enantiomer [131I](S)-I and none occurred with the (R)-enantiomer [131I](R)-I in sections from CB1 receptor knockout mice. Radioiodinated I thus appears to be a suitable radioligand for studies of CB1 cannabinoid receptors.

Journal of Medicinal Chemistry published new progress about Labeled chemical compounds Role: DGN (Diagnostic Use), PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), USES (Uses), PREP (Preparation). 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Application In Synthesis of 27483-92-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

DeVita, Robert J.’s team published research in Bioorganic & Medicinal Chemistry Letters in 1999-09-06 | CAS: 27483-92-7

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship (gonadotropin releasing hormone receptor-antagonist). 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Synthetic Route of 27483-92-7.

DeVita, Robert J. published the artcileIdentification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist, Synthetic Route of 27483-92-7, the main research area is quinolone gonadotropin releasing hormone receptor antagonist.

Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH (gonadotropin releasing hormone) receptor led to the identification of the substituted quinolone (I) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (∼300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chloro-substitution of the 1H-quinolone core.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship (gonadotropin releasing hormone receptor-antagonist). 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Synthetic Route of 27483-92-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

The important role of 27483-92-7

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 27483-92-7 is helpful to your research. Application of 27483-92-7

Application of 27483-92-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.27483-92-7, Name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, molecular formula is C7H15Cl2N. In a Patent,once mentioned of 27483-92-7

6-Aryl pyrazolo?3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 27483-92-7 is helpful to your research. Application of 27483-92-7

Reference:
Piperidine – Wikipedia,
Piperidine | C5H10946N – PubChem

 

Can You Really Do Chemisty Experiments About 27483-92-7

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 27483-92-7, and how the biochemistry of the body works.Related Products of 27483-92-7

Related Products of 27483-92-7, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.27483-92-7, Name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, molecular formula is C7H15Cl2N. In a article,once mentioned of 27483-92-7

Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (~300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chlorosubstitution of the 1H-quinolone core.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 27483-92-7, and how the biochemistry of the body works.Related Products of 27483-92-7

Reference:
Piperidine – Wikipedia,
Piperidine | C5H10944N – PubChem