Preparation and reactivity studies of 1,2-bis-triisopropylsilanylsulfanyl-alkenes
摘要:
The cross-coupling reaction of bis-triisopropylsilyl disulfide 1 on alkynes yielded 1,2-bis-triisopropylsilanylsulfanyl-alkenes 2, a new chemical class. A series of tri and tetrasubstituted olefins 2 were prepared and their behavior toward electrophiles was studied. The triisopropylsilyl groups could be readily removed by treatment with TBAF at 0 degreesC for 1 h or cesium acetate at 70 degreesC for 2 h. Soft and hard electrophiles were submitted to 2 under these conditions. The electrophiles can either react to yield double addition products with alkyl and activated halides, epoxides and acyl chlorides or cyclic adducts with chloroformate derivatives. In the latter case, 1,3-dithiol-2-ones or 1,3-dithiol-2-thiones are prepared. (C) 2001 Elsevier Science Ltd. All rights reserved.
BENITEZ F. M.; GRUNWELL J. R., J. ORG. CHEM., 1978, 43, NO 14, 2917-2918
作者:BENITEZ F. M.、 GRUNWELL J. R.
DOI:——
日期:——
CAMPTOTHECIN DRUG COMBINATIONS AND MEDICAMENTS WITH REDUCED SIDE EFFECTS
申请人:ARCH DEVELOPMENT CORPORATION
公开号:EP0768895A1
公开(公告)日:1997-04-23
[EN] CAMPTOTHECIN DRUG COMBINATIONS AND MEDICAMENTS WITH REDUCED SIDE EFFECTS<br/>[FR] COMBINAISONS MEDICAMENTEUSE CONTENANT DES CAMPTOTHECINES ET MEDICAMENTS A EFFETS SECONDAIRES REDUITS
申请人:ARCH DEVELOPMENT CORPORATION
公开号:WO1996001127A1
公开(公告)日:1996-01-18
(EN) This invention provides methods and combination formulations and kits to reduce the toxicity of camptothecin drugs, such as irinotecan (CPT-11). Disclosed are therapeutics and treatment methods employing such drugs in combination with agents that increase conjugative enzyme activity or glucuronosyltransferase activity, and agents that decrease biliary transport protein activity, such as cyclosporine A, the resultant effects of which are to decrease the significant side effects previously associated with treatment using these drugs.(FR) L'invention concerne des procédés, des formulation combinées et des kits permettant de réduire la toxicité de médicaments à la camptothécine tels que l'irinotécan (CTP-11). Elle porte également sur des procédés thérapeutiques et curatifs dans lesquels ces médicaments sont utilisés conjointement avec des agents augmentant l'activité enzymatique de conjugaison ou l'activité glucuronosyltransférase, et des agents réduisant l'activité protéique de transport biliaire tels que la cyclosporine A, ce qui a pour résultat de réduire les effets secondaires sensibles associés auparavant au traitement par ces médicaments.