180915-94-0Relevant articles and documents
A new process for the synthesis of nafoxidene as a key intermediate of lasofoxifene
Lu, Yi,Huang, Yangwei,Chen, Zhong,Lin, Yanqing,Zhao, Xueqing
, p. 6051 - 6056 (2015)
Abstract A novel brief process for the synthesis of nafoxidene has been developed. The epoxidation of 6-methoxy-1-{4-[2-(pyrrolin-1-yl)ethoxy)]phenyl}-3,4-dihydronaphthalene by m-CPBA directly gave the ketone 6-methoxy-1-[4-(2-(pyrrolidin-1-yl)ethoxy)phenyl]-3,4-dihydronaphthalen-2(1H)-one, which was subject to phenyl magnesium bromide/cerium chloride and subsequently treated with an acid to yield nafoxidene. In addition, the preparation of the starting naphthalene was also optimized by replacing the aromatic lithium at low temperature with its Grignard reagent at refluxing THF. This mild process, without the use of toxic or noble metals, was more cost-efficient and easily worked up.
Pharmaceutical composition and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and an estrogen agonist/antagonist
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Page/Page column 22, (2010/02/11)
The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a 2-alkylidene-19-nor-vitamin D derivative and an estrogen agonistlantagonist or a pharmaceuticall
Estrogen agonists/antagonists
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, (2008/06/13)
Compounds of formula A inhibit bone resorption and bone turnover, prevent bone loss, preserve bone strength and decrease serum cholesterol without causing prostate hypertrophy in male mammals: and E and B are selected from CH and N. R4 is H, OH, F or Cl.