首页> 外国专利> Process for synthesizing N-(2-(R)-hydroxy-1-(S)-indanyl)-2(R)-phenylmethyl-4(S)-hydroxy-5-(1-(4-(3-pyridylmethyl)-2(S)-N -(tert-butylcarboxamido)piperazinyl)pentane amide

Process for synthesizing N-(2-(R)-hydroxy-1-(S)-indanyl)-2(R)-phenylmethyl-4(S)-hydroxy-5-(1-(4-(3-pyridylmethyl)-2(S)-N -(tert-butylcarboxamido)piperazinyl)pentane amide

机译:N-(2-(R)-羟基-1-(S)-茚满基)-2(R)-苯甲基-4(S)-羟基-5-(1-(4-(3-吡啶基甲基))的合成方法-2(S)-N-(叔丁基羧酰胺基)哌嗪基)戊烷酰胺

摘要

In the present invention there is disclosed a process for synthesizing N-(2-(R)-hydroxy-1-(S)-indanyl)-2(R)-phenylmethyl-4(S)-hydroxy-5-(1-(4-(3-pyridylmethyl)-2(S)-N'-(tert-butylcarboxamido)piperazinyl)pentane amide of the general formula J or a hydrate thereof, which process comprises the steps of: (a) reacting for at least 5 minutes in suitable solvent one equivalent of the compound of the general formula II having the structure with excess 3-pyridine carboxaldehyde in the presence of excess reducing agent, at a temperature range of between about -78 degC and about 90 degC; (b) isolating the compound J or a hydrate thereof.
机译:在本发明中,公开了一种合成N-(2-(R)-羟基-1-(S)-茚满基)-2(R)-苯甲基-4(S)-羟基-5-(1-)的方法。通式J的(4-(3-吡啶基甲基)-2(S)-N'-(叔丁基羧酰胺基)哌嗪基)戊烷酰胺或其水合物,该方法包括以下步骤:(a)反应至少在过量的还原剂存在下,在约-78摄氏度至约90摄氏度之间的温度范围内,在合适的溶剂中5分钟一当量的通式II的通式II化合物的结构与过量的3-吡啶吡啶甲醛;分离化合物J或其水合物。

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