发明名称 Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
摘要 Synthons for the synthesis of phosphonates prodrugs POM and POC, especially for direct Cross Metathesis.
申请公布号 US8785629(B2) 申请公布日期 2014.07.22
申请号 US201013377652 申请日期 2010.06.17
申请人 Centre National de la Recherche Scientifique;Universite d'Orleans 发明人 Agrofoglio Luigi A.;Roy Vincent;Pradere Ugo
分类号 C07F9/06;C07F9/40 主分类号 C07F9/06
代理机构 Young & Thompson 代理人 Young & Thompson
主权项 1. A compound of formula (I)wherein R represents a group of formula (1) wherein R1 represents H, a straight or branched (C1-C6) alkyl group or a —(CH2)m—R2 group with R2 selected from the group consisting of hydrogen, halogen, OH, N3, NH2, epoxy groups, leaving groups and carbonyl groups and m is an integer from 0 to 5, represents a double or a triple bond,p being equal to 0 when is a triple bond and equal to 1 when is a double bond or,R=R2 with R2 selected from the group consisting of hydrogen, halogen, OH, N3, NH2, epoxy groups and analogs, leaving groups, leaving groups involved into a transmetalation step catalyzed by Pd(0), and carbonyl groups, n is an integer from 0 to 5 X and Y independently of each other represent hydrogen, halogen or a straight or branched (C1-C6)alkyl group or an hydroxymethyl group, and R′ and R″ independently of each other represent a group selected from the group consisting of an oxymethylcarbonyl group of formula (2) whereinR1 and R′1 are independently of each other hydrogen or (C1-C4)alkyl group andR′2 is a straight or branched (C1-C6)alkyl group or straight or branched (C1-C6)alkoxy groupwith the proviso that when R is cis-propenyl  n=0 and R′2 is methyl, then R1 and R′1 are not simultaneously hydrogen,a thioethylcarbonyl group of formula (3) whereinR3 is a straight or branched (C1-C6) alkyl groupa lipohilic chain selected from the group consisting of hexadecyloxypropyl (HDP)-, octadecyloxyethyl-, oleyloxypropyl-, and oleyloxyethyl-esters with the proviso that when n=0 then R is not the cis-propenyl  orR′ and R″ form with the phosphate atom to which they are linked a cycloalkyle group of formula (4) wherein R4, R5, R6, and R7 each independently represent a straight or branched (C1-C6)alkyl or aryl group or R4 and R7 independently represent a straight or branched (C1-C6) alkyl or aryl group or R5 and R6 form together an aromatic ring, said aromatic ring being optionally substitutedwith the proviso that are excluded.
地址 Paris FR