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Procedure for the preparation of an intermediate for mu opiate receptor antagonists

机译:鸦片受体拮抗剂中间体的制备方法

摘要

A process for preparing a compound of formula 1, which has the chemical name 3-endo- (8-azabicyclo [3.2.1] oct-3-yl) benzamide, or a salt thereof: ** Formula ** the process it comprises hydrogenating a compound of formula 2, which has the chemical name 3- (8-azabicyclo [3.2.1] oct-2-en-3-yl) benzamide: ** Formula ** or an acid salt thereof, in the presence of a palladium metal catalyst and, when the compound of formula 2 is in the form of a free base, in the presence of an acid, to provide a compound of formula 1 or a salt thereof, wherein the compound of formula 2 or acid salt thereof has been prepared by deprotecting a compound of formula 3: wherein: P 1 is tert-butoxycarbonyl or p-methoxybenzyloxycarbonyl.
机译:具有化学名称3-内-(8-氮杂双环[3.2.1]辛-3-基)苯甲酰胺的式1化合物的制备方法,或其盐:**式**该方法包括:在存在下,将化学名称为3-(8-氮杂双环[3.2.1] oct-2-en-3-yl)苯甲酰胺的式2化合物或其式的盐氢化。钯金属催化剂,并且当式2的化合物为游离碱形式时,在酸的存在下,提供式1的化合物或其盐,其中式2的化合物或其酸盐通过对式3的化合物进行脱保护来制备α2,其中:P 1是叔丁氧基羰基或对甲氧基苄氧基羰基。

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