公开(公告)号：WO1997035824A1

公开(公告)日：1997-10-02

申请号：PCT/JP1997000881

申请日：1997-03-18

Applicant: CHICHIBU ONODA CEMENT CORPORATION ,  NUKUI, Kazunori ,  FUKAMI, Shinji ,  KAWADA, Kosuke

Inventor： CHICHIBU ONODA CEMENT CORPORATION

IPC: C07C45/63

CPC classification number: C07J1/0011 ,  C07B39/00 ,  C07C45/63 ,  C07C67/307 ,  C07C205/43 ,  C07C205/45 ,  C07C69/716 ,  C07C47/14 ,  C07C49/16 ,  C07C49/227 ,  C07C49/457 ,  C07C49/687 ,  C07C49/80 ,  C07C69/738 ,  C07C69/757

Abstract: A process for the preparation of fluorinated dicarbonyl compounds of general formula (2), comprising reacting dicarbonyl compounds of general formula (1) with fluorine gas without any solvent in the presence of one or more acids selected from among trifluoromethanesulfonic acid, methanesulfonic acid, hydrofluoric acid, sulfuric acid, trifluoroacetic acid, boron trifluoride and sulfonated polymers wherein R , R and R are each hydrogen, alkyl or the like; and R , R and R are each the same as defined for R , R and R , or alternatively when R , R and R are each hydrogen, the hydrogen may be replaced by fluorine, while when R , R and R are each optionally substituted alkyl, one or more hydrogen atoms on the alpha -position carbon atom to the CO-group may be replaced by fluorine. This process can give fluorinated dicarbonyl compounds in high yields and at high selectivity.

Abstract translation: 一种制备通式（2）的氟化二羰基化合物的方法，包括在一种或多种选自三氟甲磺酸，甲磺酸，氢氟酸的酸的存在下，将通式（1）的二羰基化合物与氟气反应而不用任何溶剂 酸，硫酸，三氟乙酸，三氟化硼和磺化聚合物，其中R 1，R 2和R 3各自为氢，烷基等; 和R 1a，R 2a和R 3a各自与R 1，R 2和R 3所定义的相同，或者当R 1，R 2和 R 3各自为氢，氢可以被氟取代，而当R 1，R 2和R 3各自为任意取代的烷基时，α位碳原子上的一个或多个氢原子 对CO组可被氟代替。 该方法可以高产率和高选择性得到氟化二羰基化合物。

公开(公告)号：WO1996034862A1

公开(公告)日：1996-11-07

申请号：PCT/US1996006247

申请日：1996-05-03

Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH ,  DANISHEFSKY, Samuel, J. ,  MASTERS, John ,  YOUNG, Wendy ,  LINK, J., Thomas ,  ISAACS, Richard ,  SNYDER, Lawrence, B.

Inventor： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH

IPC: C07D305/14

CPC classification number: C07D493/08 ,  C07C45/29 ,  C07C45/59 ,  C07C49/613 ,  C07C49/687 ,  C07C49/713 ,  C07C49/723 ,  C07C49/737 ,  C07C49/747 ,  C07C49/753 ,  C07C49/757 ,  C07C255/31 ,  C07C255/46 ,  C07C2601/14 ,  C07C2601/16 ,  C07D305/14 ,  C07D317/72 ,  C07F7/1804

Abstract: The present invention provides three basic routes for the total synthesis of taxol having the structure (I). The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.

Abstract translation: 本发明提供了具有结构（I）的紫杉醇的全合成的三条基本路线。 本发明还提供了在上述方法中制备的中间体，用于合成这些中间体的方法以及紫杉醇和诺泰莫酚的类似物。

公开(公告)号：WO1995001960A1

公开(公告)日：1995-01-19

申请号：PCT/EP1994002294

申请日：1994-07-07

Applicant: LABORATOIRE THERAMEX S.A. ,  BOUILLON, Roger ,  VANDEWALLE, Maurits ,  DE CLERCQ, Pierre, Jean

Inventor： LABORATOIRE THERAMEX S.A.

IPC: C07C401/00

CPC classification number: C07C47/198 ,  C07C35/22 ,  C07C35/27 ,  C07C47/192 ,  C07C47/36 ,  C07C47/37 ,  C07C49/242 ,  C07C49/517 ,  C07C49/687 ,  C07C49/743 ,  C07C49/755 ,  C07C57/26 ,  C07C59/01 ,  C07C401/00

Abstract: The present invention relates to analogues of vitamin D, which lack the combined presence of the trans-fused six-membered C-ring and of five-membered D-ring, but still possess a central part consisting of a subsituted chain of five atoms, atoms which correspond to positions 8, 14, 13, 17 and 20 of vitamin D, and at the ends of which are connected, at position 20 a structural moiety representing part of the side-chain of vitamin D or of an analogue of vitamin D, and at position 8 the DELTA (5,7)-diene moiety connected to the A-ring of the active 1-alpha-hydroxy metabolite or of an established vitamin D analogue, to their preparation process, to preparation intermediates, to pharmaceutical preparations comprising these compounds and to their use in medicine.

Abstract translation: 本发明涉及维生素D的类似物，其缺乏反式融合的六元C-环和五元D环的组合存在，但仍具有由五个原子的取代链构成的中心部分， 对应于维生素D的位置8,14,13,17和20的原子，并且其末端连接在20位，代表部分维生素D的侧链或维生素D的类似物的结构部分 ，并且在位置8将与活性1-α-羟基代谢物或已建立的维生素D类似物的A环相连的DELTA（5,7） - 二烯部分，其制备方法制备中间体至药物制剂 包括这些化合物及其在药物中的用途。

公开(公告)号：WO1994005617A1

公开(公告)日：1994-03-17

申请号：PCT/US1993008061

申请日：1993-08-25

Applicant: NEW YORK UNIVERSITY

Inventor： NEW YORK UNIVERSITY ,  MCNELIS, Edward

IPC: C07C45/30

CPC classification number: C07C49/813 ,  C07C35/29 ,  C07C45/512 ,  C07C45/65 ,  C07C45/68 ,  C07C47/24 ,  C07C49/227 ,  C07C49/23 ,  C07C49/235 ,  C07C49/687 ,  C07C49/693 ,  C07C49/697 ,  C07C49/798

Abstract: Alternative methods for synthesizing haloenones and haloalkenes and their use as starting materials for synthesis of substituted or unsubstituted alkyl and aryl substituted enones and alkenes, including tamoxifen and tamoxifen analogs, using such haloenones and haloalkenes.

Abstract translation: 用于合成卤代酮和卤代烯烃的替代方法及其用作合成取代或未取代的烷基和芳基取代的烯酮和烯烃（包括他莫昔芬和他莫昔芬类似物）的起始材料，使用这种卤代酮和卤代烯烃。