Ro-0094889, Ro-09-4889
Chemical Name: 2',3'-Di-O-acetyl-5'-deoxy-5-vinylcytidine
CAS No. 216449-60-4
项目整合开发状态: Phase I
项目研究机构: Chugai (Originator)
合成路线:Silylation of 5-iodocytosine (I) with hexamethyldisilazane,followed by condensation with 5-deoxy-1,2,3-tri-O-acetyl-D-ribofuranoside (II) in the presence of stannic chloride provided 2',3'-di-O-acetyl-5'-deoxy-5-iodocytidine (III).The title vinylcytidine derivative was then obtained by displacement of the iodine atom of (III) with tri-n-butyl(vinyl)stannane (IV) using palladium catalyst and trifurylphosphine.
📌 参考资料/链接：
参考文献标题:5'-Deoxy-cytidine derivs.
文献作者:Hattori,K.; Suda,H.; Ishikawa,T.; Shimma,N.; Kohchi,Y.; Oikawa,N.; Ishitsuka,H.(F.Hoffmann-La Roche AG)
参考来源:DE 19823484; EP 0882734; ES 2142763; FR 2763953; GB 2325931; JP 1998330395
📄 详细内容
合成路线:Silylation of 5-iodocytosine (I) with hexamethyldisilazane,followed by condensation with 5-deoxy-1,2,3-tri-O-acetyl-D-ribofuranoside (II) in the presence of stannic chloride provided 2',3'-di-O-acetyl-5'-deoxy-5-iodocytidine (III).The title vinylcytidine derivative was then obtained by displacement of the iodine atom of (III) with tri-n-butyl(vinyl)stannane (IV) using palladium catalyst and trifurylphosphine.
参考文献标题:5'-Deoxycytidine derivs.
文献作者:Ishitsuka,H.; Kohchi,Y.; Shimma,N.; Oikawa,N.; Hattori,K.; Suda,H.; Ishikawa,T.(F.Hoffmann-La Roche AG)
参考来源:EP 1060183; WO 9940099