Bristol-myers Squibb Compnay

Luca Parlanti

Jurong Yu

Junying Fan

Stephen T Wrobleski

John T Hynes

Rajeev S Bhide

Zhen-Wei Cai

Ligang Qian

John Anthony Grosso

Zhongping Shi

Stephanie Barbosa

Edward J Delaney

Francis S Gibson

Reginald O Cann

Apurba Bhattacharya

Nitinchandra Patel

A process for making aziridinyl epothilone compounds according to formula G, starting from a compound according formula C where R, R, R, R, R, R, R, R, Zand Zin formulae (G) and (C) are as defined herein. The aziridinyl epothilone compounds of formula (G) are useful for the treatment of cancer.

Processes for making epothilone compounds and analogs

A process for making epi-epothilone compounds according to formula A.1, by reacting a compound according formula C with at least one halogenating agent followed by treatment with base, where R, R, R, R, R, R, R, R, Zand Zin formulae (A.1) and (C) are as defined herein. The epi-epothilone compounds of formula (A.1) can be converted into aziridinyl epothilone compounds, which are useful for the treatment of cancer.

A method for aminating pyrrole derivatives and for preparing pyrrolotriazine compounds having the formula V, 

Method for preparing pyrrolotriazine compounds

A method for aminating pyrrole derivatives via in situ generated chloramines and for preparing pyrrolotriazine compounds having the formula III, 

Method for preparing pyrrolotriazine compounds via in situ amination of pyrroles

A process is provided for the process for preparing a pyrrolotriazine aniline p38 kinase inhibitor such as amide II by the direct aminolysis of the ester I wherein ester I is reacted with a strong organometallic base, such as hexyllithium or n-butyllithium and the desired amine such as n-propylamine to form the amide II.

Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors

The present invention relates to a process for preparing certain pyrrolotriazine compounds of the formulaand pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

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Princeton, NJ, United States of America

Luca Parlanti