Category: 1205-72-7

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

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

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 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

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

Tanaka, Akito published the artcileStudies on anti-platelet agents. IV. A series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines as novel anti-platelet agents, Formula: C12H20Cl2N2, the main research area is pyrimidine bismethoxyphenyl antiplatelet agent; vasodilatory activity pyrimidine bismethoxyphenyl; cyclooxygenase inhibitor pyrimidine bismethoxyphenyl.

The syntheses and structure-activity relationships of a series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines, designed on the basis of structural analyses of several cyclooxygenase (CO) inhibitors, and their derivatives as anti-platelet agents based on CO inhibition are described. Among them, 4,5-bis(4-methoxyphenyl)-2-morpholinopyrimidine and 4,5-bis(4-methoxyphenyl)-2-(3,5-dimethylmorpholin-4-yl)pyrimidine showed potent inhibitory activity on malondialdehyde, formed by the CO-catalyzed oxygenation of arachidonic acid (A.A.) in prostanoids, production in vitro (73.4% inhibition at 10-8 M and IC50 = 1.4 × 10-8 M, resp.). Certain compounds were also examined in ex vivo studies. Of these compounds, 4,5-bis(4-methoxyphenyl)-2-(1-methyl-1,2,3,6,-tetrahydropyrid-4-yl)pyrimidine (11a) exhibited potent and long-lasting anti-platelet activity ex vivo, i.e., 11a showed 97% inhibition of platelet aggregation induced by A.A. even 24 h after oral administration of 3.2 mg/kg in guinea pigs, and 60-70% inhibition at 6 h after lower doses (1.0 mg/kg). The ex vivo activity of 11a is more than three times that of aspirin (aspirin showed 81% inhibitory activity on platelet aggregation induced by A.A. at 6 h after oral administration at 10 mg/kg is this study). Compound 11a also showed vasodilatory activity (ED50 = 5.3 × 10-6 M, while aspirin has no vasodilatory activity at 6.0 × 10-4 M).

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

1205-72-7, 1-Benzylpiperidin-4-amine dihydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of (i?)-tetrahydro-2-furoic acid (58.5 g, 504 mmol) and oxalyl chloride(86 mL, 1.0 mol) in 100 mL CH2CI2 were refluxed for 2 hours in a flask equipped with a CaCl2 guard tube. After the solution was cooled to room temperature the solvents and excess oxalyl chloride were removed by evaporation under reduced pressure. The resulting acid chloride was dissolved in 200 mL CH2CI2 and added dropwise to a solution of 1 -benzyl-4-amino piperidine dihydrochloride (142 g, 539 mmol) and triethylamine (240 mL, 1.7 mol) in 300 mL CH2C12 cooled in an ice bath. The resulting mixture was stirred for 2 hours at room temperature and subsequently washed twice with 300 mL portions of 5% aq. NaHC03 and 300 mL saturated aq. NaCl solution, dried over Na2S04, filtered, and evaporated to dryness under reduced pressure. The solid residue was triturated with 500 mL heptanes, collected by filtration, and washed twice with 200 mL portions of heptanes. The solid was air-dried at 45 C to yield (i?)-tetrahydrofuran-2-carboxylic acid (l-benzyl-piperidin-4-yl)-amide (128 g, 88%) as an off-white solid. ^-NMR (300 MHz, CDCI3): 8 7.35-7.20 (m, 5H), 6.58 (bs, 1H), 4.29 (dd, J= 5.9, 8.4 Hz, 1H), 3.92-3.77 (m, 2H), 3.48 (s, 2H), 2.82-2.74 (m, 2H), 2.32-2.21 (m, 1H), 2.19-1.95 (m, 3H), 1.94-1.78 (m, 4H), 1.58-1.40 (m, 2H) ppm., 1205-72-7

As the paragraph descriping shows that 1205-72-7 is playing an increasingly important role.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2006/28904; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem