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发明公开
CN101993406A 光学活性的吲哚啉化合物及其制备方法 有权

光学活性的吲哚啉化合物及其制备方法
摘要：
本发明提供了光学活性吲哚啉化合物即R-5-(2-胺基丙基)-1-(3-(4-氟苯甲酰氧基)丙基)-7-氰基吲哚啉。该化合物可以作为关键中间体用于制备手性药物西洛多辛。本发明还提供了R-5-(2-胺基丙基)-1-(3-(4-氟苯甲酰氧基)丙基)-7-氰基吲哚啉的制备方法，其特征在于：以1-(3-(4-氟苯甲酰氧基)丙基)-5-(2-硝基丙基)-7-氰基吲哚啉原料制备得到1-(3-(4-氟苯甲酰氧基)丙基)-5-(2-氧代丙基)-7-氰基吲哚啉，再与便宜的手性辅剂α-苯乙胺进行不对称反应(不对称诱导率为6∶1)，再脱去保护基制得。
摘要（英）：

The invention provides an indoline compound with optical activity, namely R-5-(2-amidopropyl)-1-(3-(4-fluorine benzoyl oxygen group) propyl)-7-cyan indoline. The compound can be used as a key intermediate and used for preparing a chiral drug, namely, Silodosin. The invention also provides a preparation method of R-5-(2-amidopropyl)-1-(3-(4-fluorine benzoyl oxygen group) propyl)-7-cyan indoline, which is characterized by comprising the following steps: taking 1-(3-(4-fluorine benzoyl oxygen group) propyl)-5-(2-nitrylpropyl)-7-cyan indoline as a raw material to obtain the 1-(3-(4-fluorine benzoyl oxygen group) propyl)-5-(2-oxopropyl)-7-cyan indoline, carrying out asymmetric reaction on the 1-(3-(4-fluorine benzoyl oxygen group) propyl)-5-(2-oxopropyl)-7-cyan indoline and a cheap chiral auxiliary agent, namely alpha-phenylethylamine, wherein asymmetric inductivity is 6:1, and finally removing protective group.

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