发明名称 Process-Scale Synthesis of Urolithins
摘要 Disclosed is a method of preparing a urolithin, or an intermediate or analog thereof, having a dibenzo[b,d]pyran-6-one core. The method is especially advantageous for the large-scale preparation of urolithins or intermediates or analogs thereof. The method may optionally include the preparation of a urolithin, or an intermediate or analog thereof, as a pharmaceutically acceptable salt.
申请公布号 US2015183758(A1) 申请公布日期 2015.07.02
申请号 US201414578870 申请日期 2014.12.22
申请人 Amazentis SA 发明人 Rinsch Christopher L.;Müller Roland;Skranc Wolfgang
分类号 C07D311/80;A61K31/366;A61K33/34 主分类号 C07D311/80
代理机构 代理人
主权项 1. A method of preparing a compound of formula I, comprising the step of combining in an aqueous alkaline solvent mixture a copper-containing catalyst, a compound of formula II, and a compound of formula III, thereby forming the compound of formula I; wherein the compound of formula I is represented by: R1, R2, R3, R4, R5, R6, R7, and R8 are, independently for each occurrence, selected from the group consisting of H, alkyl, haloalkyl, heteroalkyl, alkenyl, alkynyl, halogen, and OR; wherein, if two OR are present at adjacent positions, then the two R groups taken together may represent a methylene (—CH2—) group; R is selected from the group consisting of H, lower alkyl, lower haloalkyl, acyl, aracyl, sulfate, monosaccharide, and oligosaccharide; the compound of formula II is represented by: or an alkyl or aryl ester thereof; wherein X is selected from the group consisting of Cl, Br, and I; and the compound of formula III is represented by:
地址 Ecublens CH