发明名称 Method of producing compounds having HIV integrase inhivitory activity
摘要 A process for preparing a compound represented by formula (Y1) or (Y2);;wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) wherein R1d, R2d, and R4d are as defined herein.
申请公布号 US2015038702(A1) 申请公布日期 2015.02.05
申请号 US201414518209 申请日期 2014.10.20
申请人 Shionogi & Co., Ltd. 发明人 SUMINO Yukihito;MASUI Moriyasu;YAMADA Diasuke;IKARASHI Fumiya;OKAMOTO Kazuya
分类号 C07D498/14 主分类号 C07D498/14
代理机构 代理人
主权项 1. A method of producing a compound shown by formula (Y1) or formula (Y2) or a salt thereof: (wherein Rx is carbocyclyl optionally substituted by substituent E, heterocyclyl optionally substituted by substituent E, carbocyclyl lower alkyl optionally substituted by substituent E, or heterocyclyl lower alkyl optionally substituted by substituent E, and substitutent E is as defined below) comprising a step of: (Step D) reacting the compound shown by formula (X4) or a salt thereof wherein R1d is hydrogen, halogen, lower alkyloxy optionally substituted by substituent E, carbocyclyl lower alkyloxy optionally substituted by substituent E, heterocyclyl lower alkyloxy optionally substituted by substituent E, or —OSi(R1e)3, R1es are each independently lower alkyl optionally substituted by substituent E, carbocyclyl optionally substituted by substituent E, heterocyclyl optionally substituted by substituent E, carbocyclyl lower alkyl optionally substituted by substituent E, or heterocyclyl lower alkyl optionally substituted by substituent E, R2d is hydrogen, lower alkyl optionally substituted by substituent E, carbocyclyl lower alkyl optionally substituted by substituent E, or heterocyclyl lower alkyl optionally substituted by substituent E, R4d is lower alkyl optionally substituted by substituent E, carbocyclyl lower alkyl optionally substituted by substituent E, or heterocyclyl lower alkyl optionally substituted by substituent E, R6d is lower alkyl optionally substituted by substituent E, or lower alkenyl optionally substituted by substituent E, Substituent E: halogen, cyano, hydroxyl, carboxy, formyl, amino, oxo, nitro, lower alkyl, halogeno lower alkyl, lower alkyloxy, carbocyclyl optionally substituted by substituent F, heterocyclyl optionally substituted by substituent F, carbocyclyl lower alkyloxy optionally substituted by substituent F, heterocyclyl lower alkyloxy optionally substituted by substituent F, carbocyclyl lower alkylthio optionally substituted by substituent F, heterocyclyl lower alkylthio substituted by substituent F, carbocyclyl lower alkylamino optionally substituted by substituent F, heterocyclyl lower alkylamino optionally substituted by substituent F, carbocyclyloxy optionally substituted by substituent F, heterocyclyloxy optionally substituted by substituent F, carbocyclylcarbonyl optionally substituted by substituent F, heterocyclylcarbonyl optionally substituted by substituent F, carbocyclylaminocarbonyl optionally substituted by substituent F, heterocyclylaminocarbonyl optionally substituted by substituent F, halogeno lower alkyloxy, lower alkyloxy lower alkyl, lower alkyloxy lower alkyloxy, lower alkylcarbonyl, lower alkyloxycarbonyl, lower alkyloxy carbonylamino, lower alkylamino, lower alkylcarbonylamino, lower alkylaminocarbonyl, lower alkylsulfonyl, and lower alkylsulfornylamino; Substituent F: halogeno, hydroxyl, carboxy, amino, oxo, nitro, lower alkyl, halogeno lower alkyl, lower alkyloxy, and amino protecting group; with (R)-3-amino-butan-1-ol, or (S)-2-amino-propan-1-ol to obtain a compound shown by formula (X5) or formula (X5′): or a salt thereof; (Step E) reacting the compound shown by formula (X5) or formula (X5′), or a salt thereof with a compound shown by formula (V6), or a salt thereof: (wherein Rx is as defined above) to obtain a compound shown by formula (X6) or formula (X6′), or a salt thereof: and (Step F) reacting the compound shown by formula (X6) or formula (X6′), or a salt thereof to obtain the compound shown by formula (Y1) or formula (Y2) or a salt thereof.
地址 Osaka-shi Osaka JP