Tag: M.W=250-300

Moragues, J. published the artcileDopaminergic activity in a series of N-substituted 2-aminopyrimidines, COA of Formula: C12H20Cl2N2, the main research area is aminopyrimidine derivative preparation dopaminergic; structure activity aminopyrimidine derivative dopaminergic.

Twenty-four title compounds, most of the structure I (R and R1 = H or Me; R2 = H, Cl, or OMe; R3 = H, Cl, Me, or OMe; or R2R3 = OCH2O), were synthesized and tested for pharmacol. activity associated with stimulation of central and peripheral dopamine receptors using piribedil as the reference standard Most of the new compounds had some degree of dopaminergic activity although in many cases central activity was not accompanied by peripheral activity and vice versa. Structure-activity relations were not apparent, and none of the new compounds possessed dopamine receptor blocking properties.

Farmaco, Edizione Scientifica published new progress about aminopyrimidine derivative preparation dopaminergic; structure activity aminopyrimidine derivative dopaminergic. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, COA of Formula: C12H20Cl2N2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Tantry, Subramanyam J. published the artcileWhole cell screen based identification of spiropiperidines with potent antitubercular properties, Recommanded Product: tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, the main research area is spiropiperidine antitubercular; Antimycobacterial; Hypoxic conditions; MmpL3; Non-replicating phase; Whole cell screen; ss18b.

Whole cell based screens to identify hits against Mycobacterium tuberculosis (Mtb), carried out under replicating and non-replicating (NRP) conditions, resulted in the identification of multiple, novel but structurally related spiropiperidines with potent antitubercular properties. These compounds could be further classified into three classes, namely, 3-(3-aryl-1,2,4-oxadiazol-5-yl)-1′-alkylspiro[indene-1,4′-piperidine] (abbr. spiroindenes), 4-(3-aryl-1,2,4-oxadiazol-5-yl)-1′-alkylspiro[chromene-2,4′-piperidine] (abbr. spirochromenes) and 1′-benzylspiro[indole-1,4′-piperidin]-2(1H)-one (abbr. spiroindolones). Spiroindenes showed ≥4 log10 kill (at 2-12 μM) on replicating Mtb, but were moderately active under non replicating conditions. Whole genome sequencing efforts of spiroindene-resistant mutants resulted in the identification of the I292L mutation in MmpL3 (Mycobacterial membrane protein Large), required for the assembly of mycolic acid into the cell wall core of Mtb. MIC modulation studies demonstrated that the mutants were cross-resistant to spirochromenes but not to spiroindolones. This paper describes lead identification efforts to improve potency while reducing the lipophilicity and hERG liabilities of spiroindenes. Addnl., as deduced from the SAR studies, the authors provide insights regarding the new chem. opportunities that the spiroindolones can offer to the TB drug discovery initiatives.

Bioorganic & Medicinal Chemistry Letters published new progress about Mutation. 137419-24-0 belongs to class piperidines, name is tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, and the molecular formula is C18H23NO2, Recommanded Product: tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Agarwal, Jyoti published the artcileWater-mediated, highly-efficient and improved protocol for the synthesis of vesamicol, its analogues and β-blockers through the highly-chemoselective aminolysis of epoxides, COA of Formula: C18H23NO2, the main research area is vesamicol analog green preparation diastereoselective; epoxide aryl piperidine chemoselective aminolysis water mediated.

An efficient, eco-friendly and cost-effective protocol was developed for the synthesis of vesamicol e.g., I, benzovesamicol, spirovesamicol, their analogs and drug mols. such as Naftopidil and SR 59230 A. In this reaction, water had played dual role i.e. of bifunctional catalyst and reaction medium, also no other chem. reagent/promotor was required to afford the products. Reaction follows 100% atom economy and was found to be highly chemo-selective. All studied reactions worked well to yield the corresponding products in excellent to near quant. yields without following the tedious and time consuming column chromatog. as purification step. Thus, this protocol provided the vesamicol and other products without generating any chem. waste to the environment.

ChemistrySelect published new progress about Aminolysis. 137419-24-0 belongs to class piperidines, name is tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, and the molecular formula is C18H23NO2, COA of Formula: C18H23NO2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Peindy N’Dongo, Harmel W. published the artcilePreparation and biological evaluation of cyclopentadienyl-based 99mTc-complexes [(Cp-R)99mTc(CO)3] mimicking benzamides for malignant melanoma targeting, Quality Control of 1205-72-7, the main research area is cyclopentadienyl technetium 99m complex preparation melanoma imaging.

The biol. evaluation of half-sandwich 99mTc-complexes that surrogate iodobenzamide with a high affinity for melanin tumor tissue is described. We have synthesized via retro Diels-Alder reaction two models of 99mTc complexes which possess the piano stool [Cp99mTc(CO)3] motif instead of a Ph ring as in the original iodobenzamide 123I-N-(N-benzylpiperidin-4-yl)-2-iodobenzamide (2-IBP) and N-(2-diethylaminoethyl)-4-iodobenzamide (BZA). Diels-Alder products 2a-2b (HCp-CONHR)2 (2a, R=2-diethylaminoethyl; 2b, R=benzylpiperidin-4-yl) were prepared and reacted with fac-[99mTc(H2O)3(CO)3]+ 1 in water to produce the corresponding 99mTc complexes [(2a)99mTc(CO)3] 4a and [(2b)99mTc(CO)3] 4b. The structures of the 99mTc complexes on the no-carrier-added level have been confirmed by chromatog. comparison with the corresponding rhenium complexes and, macroscopically characterized by IR, NMR, ESI-MS and X-ray crystallog. for [triclinic, P-1, a=7.3518(1) Å, b=8.0309(2) Å, c=17.5536(3) Å, α=99.1260(5)°, β=90.4215(14)°, γ=117.0187(11)°]. The radioconjugate showed good in vitro stability. In murine melanoma B16F1 cells, significant cellular uptake (43.9% of the total applied activity) was attained after 4 h at 37°C with about 50% of the cell-associated radioactivity being internalized in the cells (22% of the applied activity). Furthermore, in melanoma-bearing C57BL6 mice, tumor uptake values of 3.39±0.50 %ID g-1 and 3.21±0.26 %ID g-1 at 1 and 4 h postinjection, resp., were observed indicating a good retention of in the tumor.

Nuclear Medicine and Biology published new progress about Melanoma. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Quality Control of 1205-72-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Valenta, Vladimir published the artcilePotential neuroleptics of the orthopramide series; synthesis of heterocyclic 5-amino-2-methoxybenzamides and of some related compounds, Name: 1-Benzylpiperidin-4-amine dihydrochloride, the main research area is neuroleptic aminomethoxybenzamide heterocyclic preparation.

Condensation of 2,5-MeO(O2N)C6H3COCl with heterocyclic amines and hydrazines gave the title derivatives I (R = NO2, n = 0, 1) and II (R = NO2; Z = NH, X = CH, N; Z = bond, X = N). Reduction of I and II (R = NO2) with Raney Ni gave amino derivatives I and II (R = NH2). I (R = NHMe, n = 1) and II (R = NHMe, Z = NH, X = CH) were prepared via tosyl derivatives All prepared compounds I and II were tested as potential neuroleptics. Only compounds II (Z = NH, X = CH) show mild activity.

Collection of Czechoslovak Chemical Communications published new progress about Tranquilizers. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Name: 1-Benzylpiperidin-4-amine dihydrochloride.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chambers, Mark S. published the artcileSpiropiperidines as high-affinity, selective σ ligands., HPLC of Formula: 137419-24-0, the main research area is spiropiperidine selective sigma ligand; tetralin spiropiperidino selective sigma ligand; indan spiropiperidino selective sigma ligand; benzocycloheptane spiropiperidino selective sigma ligand; radioligand displacement spiropiperidinobenzocycloalkane; structure activity spiropiperidinobenzocycloalkane receptor binding.

A variety of achiral conformationally restricted spirocyclic piperidines were prepared in an attempt to investigate the functional role of the central σ recognition site. All compounds possessed a lipophilic N-substituent incorporating either a tetralin (I; n = 2, R = PhCH2, Bu, hexyl, 2-picolyl, cyclohexylmethyl, CH2CH:CH2, 2-furylmethyl, 2-thienylmethyl, CH2CH:CMe2, etc.), indan (I; n = 1, R = PhCH2, PhCH2CH2, CH2CH:CMe2, Bu, etc.), or benzocycloheptane skeleton (I; n = 3, R = PhCH2, Bu). Their in vitro affinity at the σ site was assessed in radioligand displacement experiments with guinea pig cerebellum homogenates using the σ-specific radioligand N,N-di-o-[5-3H]-tolylguanidine (II). A study of the structure-activity relationships identified the N-Bu and N-dimethylallyl substituents as the optimum groups for high affinity and selectivity at the σ site, e.g., I (n = 1, R = CH2CH:CMe2), pIC50 = 8.9 vs II and >10,000-fold selective over the dopamine D2 receptor. Such compounds are amongst the highest affinity σ ligands reported to date, with excellent selectivity over the dopamine D2 receptor, and may serve as a useful tool for exploring the physiol. role of the σ site.

Journal of Medicinal Chemistry published new progress about Antipsychotics. 137419-24-0 belongs to class piperidines, name is tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, and the molecular formula is C18H23NO2, HPLC of Formula: 137419-24-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Crider, A. Michael published the artcileSynthesis of nitrosourea derivatives of pyridine and piperidine as potential anticancer agents, HPLC of Formula: 1205-72-7, the main research area is nitrosourea piperidinyl chloroethyl; anticancer piperidinylnitrosourea.

RNHCON(NO)CH2CH2Cl (I; R = 1-benzyl-3-piperidinyl, 1-benzyl-4-piperidinyl, 1-butyl-4-piperidinyl, 1-ethyl-3-piperidinyl, 3-pyridyl) were prepared (by reaction of RNH2 with ClCH2CH2NCO followed by nitrosation of RNHCONHCH2CH2Cl) and evaluated for anticancer activity. I (R = 1-benzyl-4-piperidinyl) hydrogen maleate exhibited good activity against intracranial L1210 leukemia as well as the mouse ependymoblastoma brain tumor system. It exhibited comparable activity in the Lewis lung carcinoma system to N,N’-bis(2-chloroethyl)-N-nitrosourea. Replacement of the N-benzyl group in both the 3-piperidinyl- and 4-piperidinylnitrosoureas resulted in less active compounds in all tumor systems tested. I (R = 3-pyridyl) was inactive in the L-1210 leukemia system.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, HPLC of Formula: 1205-72-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Takai, Haruki published the artcileSynthesis of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines as potential antihypertensive agents, Application In Synthesis of 1205-72-7, the main research area is quinazolinylpiperidine antihypertensive adrenergic blocking preparation; piperidine quinazolinyl oxophenylethyl hydroxyphenethyl.

Piperidinylquinazolines, e.g. I [R = R1 = H, Cl, OMe; R = H, R1 = Cl, OMe; Z = O, (H, OH)] were prepared and tested for antihypertensive activity. I [Z = (H, OH)] were generally the most effective in lowering blood pressure in the spontaneous hypertensive rat model, and KF5908 [I, R = H, R1 = Cl, Z = (H, OH)] showed strong α-adrenergic blocking activity.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, Application In Synthesis of 1205-72-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Takai, Haruki published the artcileSynthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents, COA of Formula: C12H20Cl2N2, the main research area is quinazolinepiperidine derivative preparation antihypertensive; piperidine quinazoline derivative preparation antihypertensive.

A series of piperidine derivatives with a 2-oxo-1,2,3,4-tetrahydro-quinazoline or 2,4-dioxo-1,2,3,4-tetrahydroquinazoline ring at the 4-position were prepared and tested for antihypertensive activity in rats. Among the compds tested, I  [92311-03-0] and II  [92311-10-9] produced relatively strong hypotension in the spontaneously hypertensive rat model.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 1205-72-7 belongs to class piperidines, name is 1-Benzylpiperidin-4-amine dihydrochloride, and the molecular formula is C12H20Cl2N2, COA of Formula: C12H20Cl2N2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Takemoto, Toshiyasu published the artcileAsymmetric synthesis of enantiomerically pure spiro [((2S)-hydroxy)indane-1,4′-piperidine], Quality Control of 137419-24-0, the main research area is spirohydroxyindanepiperidine enantioselective preparation intermediate tachykinin receptor antagonist; asym synthesis enantiomerically pure spirohydroxyindanepiperidine.

Two methods for the preparation of enantiomerically pure spirohydroxyindanepiperidine (S)-I (R = H), a key intermediate for the synthesis of a tachykinin receptor antagonist, from indenepiperidine II (R = H) are described. E.g., II (R = Me3COCO, Boc) was epoxidized with methyltrioxorhenium, the epoxide opened regioselectively to the 2-indanone derivative which was oxidized with PCC and then reduced enantioselectively in the presence of an Corey-Bakshi-Shibata oxazaborolidine catalyst to give N-Boc (S)-I (R = Boc) in 100% yield and 89% ee from the 2-indanone derivative E.g., II (R = Boc) was epoxidized enantioselectively with the (R,R)-Jacobsen epoxidation catalyst to give epoxide III in 51% yield and 91% ee; III was reduced regioselectively with ammonium formate in the presence of palladium on carbon, and the Boc derivative was then deprotected with HCl in dioxane to give the hydrochloride salt of I (R = H).

Tetrahedron: Asymmetry published new progress about Epoxidation, stereoselective. 137419-24-0 belongs to class piperidines, name is tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, and the molecular formula is C18H23NO2, Quality Control of 137419-24-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem