| 摘要 |
<p>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.</p> |
