发明名称 Intermediates for the preparation of analogs of halichondrin B
摘要 Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
申请公布号 US8884031(B2) 申请公布日期 2014.11.11
申请号 US201314096549 申请日期 2013.12.04
申请人 Eisai R&D Management Co., Ltd. 发明人 Chase Charles E.;Fang Francis G.
分类号 C07D493/22;C07D493/08;C07D407/06;C07D307/33;C07D493/18;C07F7/18;C07D307/28;C07D493/20;C07D493/10;C07D493/04;C07D407/14 主分类号 C07D493/22
代理机构 Clark & Elbing LLP 代理人 Clark & Elbing LLP
主权项 1. A compound of formula or C: wherein: designates a single or double bond; n is 1, 2, or 3; each of PG5 and PG6 is independently a suitable hydroxyl protecting group; W is CH-A or C(O); A is a C1-6 aliphatic group, wherein A is optionally substituted with one or more Q1 groups; each Q1 is independently selected from cyano, halo, azido, oxo, OR, SR, SO2R, OSO2R, N(R)2, NR(CO)R, NR(CO)(CO)R, NR(CO)N(R)2, NR(CO)OR, (CO)OR, O(CO)R, (CO)N(R)2, O(CO)N(R)2, or OPG1, wherein PG1 is a suitable hydroxyl protecting group, and wherein: optionally two Q1 are on A and are taken together to form a 3-8 membered saturated, partially unsaturated, or aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each R is independently selected from hydrogen or an optionally substituted group selected from C1-6 aliphatic, a 5-10 membered saturated, partially unsaturated or aryl carbocyclic ring, or a 4-10 membered saturated, partially unsaturated or aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, wherein: when Q1 is independently selected from N(R)2, NR(CO)N(R)2, (CO)N(R)2, and O(CO)N(R)2, two R groups on the same nitrogen atom are optionally taken together with said nitrogen atom to form a 3-8 membered saturated, partially unsaturated, or aryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; and wherein XB is O, and RB is TMS; XB is H and OH, and RB is TMS; or XB is H and OAc, and RB is Ac; and R1 is —CH2CO2R2, wherein R2 is alkyl.
地址 Tokyo JP