1450879-66-9Relevant articles and documents
Enantioselective synthesis of cis -3-fluoropiperidin-4-ol, a Building block for medicinal chemistry
Shaw, Simon J.,Goff, Dane A.,Boralsky, Luke A.,Irving, Mark,Singh, Rajinder
, p. 8892 - 8897 (2013)
The first enantioselective route to both enantiomers of cis-1-Boc-3-fluoropiperidin-4-ol, a highly prized building block for medicinal chemistry, is reported. An enantioselective fluorination is employed, taking advantage of the methodology reported by MacMillan, which uses a modified cinchona alkaloid catalyst. In studying the fluorination reaction, we have shown that the catalyst can be replaced by commercially available primary amines, including α-methylbenzylamine, with similar levels of enantioselectivity. The piperidinols are readily crystallized to obtain enantiopure material.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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, (2015/02/25)
The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
-
, (2015/02/25)
The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.