28797-61-7 (哌仑西平,Pirenzepine)

哌仑西平;11-[2-(4-甲基哌嗪-1-基)乙酰基]-5H-吡啶并[2,3-b][1,4]苯并二氮杂卓-6-酮;奥卡西平;盐酸哌仑西平;吡疡平;必舒胃;哌吡氮平;哌吡卓酮;胃疡卓酮;

Pirenzepine;Gastrozepin;11-[2-(4-Methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;PIRENZEPINE DIHYDROCHLORIDE;[3H]-Piclamilast;[3H]-Pirenzepine;11-[2-(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one;3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide;3-(cyclopentyloxy)-N-(3,5-dichloropyrid-4-yl);3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide;Cpodpmb;N-(3,5-dichloro(pyridin-4-yl))(3-cyclopentyloxy-4-methoxyphenyl)carboxamide;Piclamilast;RP 73401;RP-73401;RPR 73401;PIRENZEPINE [INN];NCGC00015836-19;Tocris-1071;6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-;KBio3_002445;5,11-Dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one;PIRENZEPINE [WHO-DD];HY-17037A;HMS2089K21;NCGC00015836-10;Pirenzepine (INN);11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one;6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]- (8CI,9CI);PDSP2_000949;Pirenzepine [INN:BAN];11-((4-Methyl-1-piperazinyl)acetyl)-5,11-dihydro-6H-pyrido(2,3-b)(1,4)benzodiazepin-6-one;PIRENZEPINE [MI];ACI-91;3G0285N20N;EINECS 249-228-4;BDBM39341;Prestwick2_000129;DTXSID7023487;SPBio_001494;FT-0673943;Pirenzepinum;BRN 0628987;CAS-29868-97-1;KBio1_000127;6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-;NCGC00024297-05;BCP12188;L000485;11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride;NCGC00015836-04;Prestwick1_000129;Pirenzepina [INN-Spanish];HMS3742E07;PIRENZEPINE [VANDF];IDI1_000127;BPBio1_000196;KBioGR_000794;D08389;BSPBio_000178;11-[(4-Methyl-1-piperazinyl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one #;DB00670;NINDS_000127;C07508;NCGC00015836-03;DivK1c_000127;KBio2_004426;SDCCGSBI-0050935.P004;CAS-28797-61-7;CS-0013749;NS00006691;CHEMBL9967;cid_185248;SPBio_002117;Pirenzepin;11-(2-(4-Methylpiperazin-1-yl)acetyl)-5,11-dihydro-6H-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one;CCG-205042;WST-057;SBI-0050935.P003;NCGC00015836-07;Spectrum2_001417;AKOS015969751;starbld0016668;Q419550;BRD-K89375097-300-05-4;NCGC00015836-06;BSPBio_002945;6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-;KBio2_006994;AB00053603;FT-0600051;11-[2-(4-methylpiperazin-1-yl)ethanoyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride;NCGC00015836-09;11-[2-(4-methylpiperazin-1-yl)-acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one;28797-61-7;KBioSS_001858;SCHEMBL41705;MLS000069702;Spectrum_001378;KBio2_001858;Lopac-P-7412;NCGC00015836-12;NCGC00015836-05;CHEBI:8247;AB00053603_09;UNII-3G0285N20N;NCGC00015836-08;Spectrum4_000437;HMS3742G13;NCGC00015836-01;SMR000058502;PDSP1_000965;2-[2-(4-methylpiperazin-1-yl)acetyl]-2,4,9-triazatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-10-one;5,11-Dihydro-11-((4-methyl-1-piperazinyl)acetyl)-6H-pyrido(2,3-b)(1,4)benzodiazepin-6-one;Prestwick0_000129;LS-519;BRD-K89375097-300-06-2;Spectrum5_001344;Pirenzepinum [INN-Latin];DTXCID303487;11-[2-(4-Methyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one;Lopac0_000962;Tox21_110239;Pirenzepina;NCGC00024297-02;AB00053603-08;NCGC00015836-02;11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2, 3-b][1, 4]benzodiazepin-6-one;Prestwick3_000129;11-[2-(4-methyl-1-piperazinyl)-1-oxoethyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride;11-[2-(4-methylpiperazino)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride;Tox21_110239_1;NCGC00024297-04;Spectrum3_001453;GTPL328;2-(2-(4-methylpiperazin-1-yl)acetyl)-2,4,9-triazatricyclo(9.4.0.0^(3,8))pentadeca-1(11),3,5,7,12,14-hexaen-10-one;Pyrenzepine;Pirenzepina (INN-Spanish);Gastri p;11-((4-methylpiperazin-1-yl)acetyl)-5,11-dihydro-6H-pyrido(2,3-b)(1,4)benzodiazepin-6-one;5,11-Dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one;6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-; 6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]- (8CI,9CI); 5,11-Dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-6H-pyr;Pirenzepinum (INN-Latin);PIRENZEPINE [USAN];Pirenzepine (USAN/INN);BRD-K89375097-300-08-8;11-(2-(4-methylpiperazin-1-yl)acetyl)-5H-pyrido(2,3-b)(1,4)benzodiazepin-6-one;L-S 519;PirenzepineDihydrochlorideMonohydrate;A02BX03;Gastrozepin (TN);

MFCD31726295

RMHMFHUVIITRHF-UHFFFAOYSA-N

1S/C19H21N5O2/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24/h2-8H,9-13H2,1H3,(H,21,26)

O=C(CN1CCN(C)CC1)N1C2=C(C=CC=N2)NC(C2C=CC=CC1=2)=O

249-228-4

选择性抗胆碱药,可阻断胆碱受体,减少胃酸和胃蛋白酶的分泌,并能解除平滑肌的痉挛与痛感。对胃粘膜的M受体作用强,而对平滑肌、心肌和唾液腺等的M受体作用小,因而对心脏、瞳孔、唾液腺、胃肠平滑肌等的副作用少。临床主要用于急慢性胃和十二指肠溃疡,对胆碱型迷走神经张力过高所致的胃酸分泌过多,更为适用。

以3-氨基吡啶为原料,在80℃氯化生成3-氨基-2-氯吡啶(Ⅰ) 3.86g化合物(I)和三乙胺溶于苯,在搅拌下缓慢滴加5.85g邻硝基苯甲酰氯的苯溶液。经回流反应后,过滤。滤液浓缩,即得6.17g酰化产物(Ⅱ)的粗品,收率95%。 5.0g化合物(Ⅱ)溶于27ml乙酸,缓慢加入含过量氯化亚锡的浓盐酸溶液。加热反应后,冷却,用****处理,得4.1g还原产物(Ⅲ),收率92%,也可用催化氢化来还原。 8.0g化合物(Ⅲ),在200℃下搅拌。待环合反应完全后,冷却,用醇处理得4.1g环合产物(Ⅳ),收率60%。 3.17g化合物(Ⅳ)溶于二氧六环,同时滴加3.4ml三乙胺和1.9ml氯乙酰氯,再回流8h。过滤,滤液浓缩,所得粗品重结晶,得3.58g化合物(V),收率83%。 3.01g化合物(V)和8.2ml N-甲基哌嗪溶于60ml苯,回流18h。蒸出苯,残液用盐酸处理,得3.29g二盐酸哌仑西平粗品,收率74%。