Iontcho Radoslavov Vlahov,Hari Krishna R. Santhapuram,Paul Joseph Kleindl,Christopher Paul Leamon,Fei You
申请号：
US14388311
公开号：
US09505747B2
申请日:
2013.03.29
申请国别(地区):
US
年份:
2016
代理人:
摘要：
The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl； and R8 is C1-C6 n-alkyl； wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.
