发明名称 |
Method for producing G3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-on |
摘要 |
Preparation of 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one involves: (A) reacting 2-nitrophenylacetic acid with 4-amino-N-phenyl-methylpiperidine in the presence of a condensing agent; (B) converting the carbonyl groups of the resulting compound to methyl groups; (C) reducing and cyclizing the intermediate; and (D) splitting off the benzyl protective group. Preparation of 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-bendiazepin-2(1H)-one of formula (I) involves: (A) reacting 2-nitrophenylacetic acid with 4-amino-N-phenyl-methylpiperidine in the presence of a condensing agent; (B) converting the carbonyl groups of the resulting 2-nitro-N-[1-(phenylmethyl)-4-piperidinyl]phenylacetamide into methyl groups by addition of a reducing agent; (C) cyclizing the N-2-[2-(nitrophenyl)ethyl]-1-(phenylmethyl)-4-aminopiperidine intermediate in the presence of a condensing agent after having reduced its nitro group using a Raney-nickel catalyst; and (D) splitting off the benzyl protective group from the resulting 3-[1-(phenylmethyl)-4-piperidinyl]-2,3,4,5-tetrahydro-1,3- benzodiazepin-2(1H)-one to give compound (I). [Image] ACTIVITY : Antimigraine MECHANISM OF ACTION : CGRP antagonist. |
申请公布号 |
ZA200609919(B) |
申请公布日期 |
2008.07.30 |
申请号 |
ZA20060009919 |
申请日期 |
2006.11.28 |
申请人 |
BOEHRINGER INGELHEIM INTERNATIONAL GMBH |
发明人 |
SCHNAUBELT, JURGEN;SOYKA, RAINER;GUTSCHERA, LUDWIG;KRIIGER, THOMAS;RAIL, WERNER;BIRK, NORBERT;HEIMROTH, HEIDELORE;PROELL, ARMIN |
分类号 |
C07D |
主分类号 |
C07D |
代理机构 |
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代理人 |
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主权项 |
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