发明名称 Methods of preparing toll-like receptor modulators
摘要 The present invention provides methods of preparing 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one and related compounds.
申请公布号 US9573952(B2) 申请公布日期 2017.02.21
申请号 US201514853883 申请日期 2015.09.14
申请人 Gilead Sciences, Inc. 发明人 Allen Darin;Brown Brandon Heath;Chao Jessica Jade;Halcomb Randall L.;Hrvatin Paul;McFadden Ryan;Roethle Paul;Rudio Erwina;Yang Hong;Yu Richard Hung Chiu
分类号 C07D247/02;C07D475/06;C07D207/09;C07D239/47;C07D239/46;C07D239/48;C07D239/545;C07D487/04;C07D207/06 主分类号 C07D247/02
代理机构 代理人 Marquart Timothy A.
主权项 1. A method of making a compound of Formula Ia:comprising: (a) forming a first reaction mixture comprising a compound of Formula IIa: a non nucleophilic base, a first solvent, and a compound of Formula IIIa: under conditions suitable to form a compound of Formula IVa:  and (b) forming a second reaction mixture comprising the compound of Formula IVa, a second solvent and a reducing agent under conditions suitable to prepare the compound of Formula I,wherein R1 and R11 are each independently C1-C6 alkyl; and LG is selected from the group consisting of halogen, —OH, and —OSO2R13, wherein R13 is selected from the group consisting of C1-C6 alkyl, C1-C6 haloalkyl and aryl, wherein the aryl group is substituted with 1 to 3 R13a groups each independently selected from the group consisting of C1-C6 alkyl, halogen, and NO2.
地址 Foster City CA US