发明名称 SYNTHETIC INTERMEDIATE OF 1-(2-DEOXY-2-FLUORO-4-THIO-ß-D-ARABINOFURANOSYL)CYTOSINE, SYNTHETIC INTERMEDIATE OF THIONUCLEOSIDE, AND METHOD FOR PRODUCING THE SAME
摘要 A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.;
申请公布号 US2016362389(A1) 申请公布日期 2016.12.15
申请号 US201615246177 申请日期 2016.08.24
申请人 FUJIFILM Corporation 发明人 NAKAMURA Kouki;SHIMAMURA Satoshi;IMOTO Junichi;TAKAHASHI Motomasa;WATANABE Katsuyuki;WADA Kenji;FUJINO Yuuta;MATSUMOTO Takuya;TAKAHASHI Makoto;OKADA Hideki;YAMANE Takehiro;ITO Takayuki
分类号 C07D333/32;C07C309/73;C07C47/277;C07H7/04;C07H13/04;C07C309/66;C07C69/78;C07C69/618;C07C69/76;C07C69/28;C07C69/96;C07F7/18;C07C251/38;C07C251/40 主分类号 C07D333/32
代理机构 代理人
主权项 1. A compound represented by the following formula [1F]: (wherein R1 represents a hydroxyl-protecting group; R2 represents a hydroxyl-protecting group; or R1 and R2 may together form an optionally substituted C1-3 alkylene group; and R3C represents a hydrogen atom, a halogen atom, a group represented by the following formula [16]: OR3a  [16┘ (wherein R3a represents a hydroxyl-protecting group), or an optionally substituted C1-6 alkyl group; R3D represents a hydrogen atom, a halogen atom, a group represented by the following formula [16] OR3a  [16┘ (wherein R3a has the same meanings as those described above), or an optionally substituted C1-6 alkyl group; R4 represents a halogen atom, a hydroxyl group, an optionally substituted C1-6 alkylsulfonyloxy group or an optionally substituted arylsulfonyloxy group; R5 and R6 together represent a group represented by the following formula [2]: ═Y  [2┘ (wherein Y represents an oxygen atom or a group represented by the following formula [3]: ═N—OR7  [3┘ (wherein R7 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclic group or an optionally substituted silyl group)); or R4 and R5 together represent a sulfur atom; and R6 represents a hydroxyl group, provided that, when R5 and R6 together represent a group represented by the following formula [2a]: ═O  [2a┘, one of R3C and R3D represents a halogen atom, the other represents a hydrogen atom, and R4 represents a halogen atom, an optionally substituted C1-6 alkylsulfonyloxy group or an optionally substituted arylsulfonyloxy group; when R4 and R5 together represent a sulfur atom and one of R3C and R3D represents a hydrogen atom, the other represents a halogen atom, or an optionally substituted C1-6 alkyl group; when R5 and R6 together represent a group represented by the following formula [3]: ═N—OR7  [3┘ (wherein R7 has the same meanings as those described above), one of R3C and R3D represents a group represented by the following formula [16]: OR3a  [6┘ (wherein R3a has the same meanings as those described above), the other represents a hydrogen atom, and R4 represents an iodine atom, a hydroxyl group, an optionally substituted C1-6 alkylsulfonyloxy group or an optionally substituted arylsulfonyloxy group, R1 represents an optionally substituted acyl group, and R2 represents an optionally substituted acyl group; and when R5 and R6 together represent a group represented by the following formula [3]: ═N—OR7  [3┘ (wherein R7 has the same meanings as those described above), one of R3C and R3D represents a hydrogen atom, the other represents a hydrogen atom, and R4 represents a hydroxyl group, R1 represents an optionally substituted aroyl group, and R2 represents an optionally substituted aroyl group).
地址 Tokyo JP