Method for preparation of taxol using an oxazinone

Details Method for preparation of taxol using an oxazinone Method for preparation of taxol using an oxazinone

C - Chemistry, Metallurgy

07

D

260/368, 260/244

C07D 305/14 (2006.01) C07C 233/87 (2006.01) C07D 265/06 (2006.01)

Patent

CA 2029787

Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: (see formula 1) wherein R1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR7 wherein R7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R2 and R5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR8 wherein R8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R3 and R6 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.

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