阅读说明：本技术 供给一氧化氮的***素类似物的制备方法 (Nitric oxide donating prostaglandin analogs ) 是由 N·阿尔米兰特 于 2019-02-12 设计创作，主要内容包括：本发明涉及制备式(I)的己酸,6-(硝基氧基)-,(1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(乙基氨基)-7-氧代-2-庚烯-1-基]-3,5-二羟基环戊基]-1-(2-苯基乙基)-2-丙烯-1-基酯的方法。根据本发明,通过使硼酸酯保护形式的比马前列素与6-(硝基氧基)己酰氯偶联和除去硼酸酯保护基,可以以高纯度有效地制备化合物(I)。6-(硝基氧基)己酰氯中间体通过2-己内酯的开环反应、随后用HNO<Sub>3</Sub>和H<Sub>2</Sub>SO<Sub>4</Sub>的混合物在二氯甲烷中使6-羟基己酸钾盐硝化来制备。<Image he="665" wi="700" file="DDA0002637969630000011.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"></Image>(The present invention relates to a process for the preparation of hexanoic acid of formula (I), 6- (nitrooxy) -, (1S,2E) -3- [ (1R,2R,3S,5R) -2- [ (2Z) -7- (ethylamino) -7-oxo-2-hepten-1-yl]-3, 5-dihydroxycyclopentyl]-1- (2-phenylethyl) -2-propen-1-yl ester. According to the present invention, compound (I) can be efficiently produced with high purity by coupling bimatoprost in a borate-protected form with 6- (nitrooxy) hexanoyl chloride and removing the borate protecting group. 6- (Nitroxy) hexanoyl chloride intermediate by ring opening of 2-caprolactone followed by HNO 3 And H 2 SO 4 Is prepared by nitrating potassium 6-hydroxycaproate in dichloromethane.)