公开(公告)号：US5079349A

公开(公告)日：1992-01-07

申请号：US473537

申请日：1990-02-01

Applicant: Johan W. Scheeren ,  Joannes F. M. De Bie ,  Dirk De Vos

Inventor： Johan W. Scheeren ,  Joannes F. M. De Bie ,  Dirk De Vos

IPC: C07F7/08

CPC classification number: C07F7/0818

Abstract: The invention relates to novel compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof.Daunomycinone can be used for the preparation of daunomycin and adriamycin.

公开(公告)号：US5294701A

公开(公告)日：1994-03-15

申请号：US879737

申请日：1992-05-06

Applicant: Johan W. Scheeren ,  Joannes F. M. de Bie ,  Dirk de Vos

Inventor： Johan W. Scheeren ,  Joannes F. M. de Bie ,  Dirk de Vos

IPC: A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07D221/18 ,  C07F7/08 ,  C07H15/24 ,  C07H15/244 ,  C07H15/252 ,  C07H15/26 ,  C07H17/02

CPC classification number: C07H15/252 ,  C07D221/18 ,  C07F7/0812 ,  C07F7/0818 ,  C07H15/244 ,  C07H17/02

Abstract: This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.

Abstract translation: 本发明提供了新颖的抗肿瘤化合物，其中R1和R2是氢或一起形成任选地含有N原子作为杂原子的烷基，烷氧基或OH取代的芳族基团; R是-COCH 3或-C 3位C-R 4，R 4是H或三甲基甲硅烷基; 并且R 3是H或-COCF 3; 及其酸加成盐; 以及含有这些化合物的组合物。