- A new process for the synthesis of nafoxidene as a key intermediate of lasofoxifene
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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.
- Lu, Yi,Huang, Yangwei,Chen, Zhong,Lin, Yanqing,Zhao, Xueqing
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- A PROCESS FOR THE PREPARATION OF LASOFOXIFENE TARTRATE
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The present invention relates to solid state chemistry of 1-(2-[4-(6-methoxy-3,4-dihydronaphthalene-1-yl) phenoxy]ethyl)pyrrolidine, a process for its preparation and its use as an intermediate in the synthesis of lasofoxifene.
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Page/Page column 19; 20
(2010/11/17)
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- Pharmaceutical composition and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and an estrogen agonist/antagonist
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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
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Page/Page column 22
(2010/02/11)
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- Estrogen agonists/antagonists
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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.
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- Estrogen agonists/antagonists
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Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
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- 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis
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Compounds of this formula STR1 are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
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