140375-21-9Relevant articles and documents
Crystallization engineering in aza-steroid: Application in the development of finasteride
Bhattacharya, Apurba,Manudhane, Kushal S,Maddula, Srinivasula Reddy,Sreekanth,Thota, Sridhar,Bandichhor, Rakeshwar
, p. 599 - 602 (2013)
Novel and robust crystallization approach based on solid solution formation was developed for the purification of finasteride. This is an unprecedented approach that describes the use of pure finasteride 1 to purify different lots of finasteride 1 (impure) contaminated with dihydrofinasteride 2.
New approach to 3-oxo-4-aza-5α-androst-1-ene-17β-(N-tert- butylcarboxamide)
Jiang, Zhong-Xing,Ye, Jing-Quan,Jiang, Li,Zhao, Ying-Sheng
, p. 690 - 693 (2005)
We describe the synthesis of 3-oxo-4-aza-5α-androst-1-ene-17β- (N-tert-butylcarboxamide) (finasteride) from 4-androstene-3,17-dione (AD) in seven steps in an overall yield of 18.6% via oxidation, ammoniumation, dehydration, and dehydrogenation.
Method for forming double bonds between 1-position and 2-position during synthesis of finasteride and dutasteride
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, (2016/12/01)
The invention provides a method for forming double bonds between the 1-position and the 2-position during synthesis of finasteride and dutasteride. According to the process, a dihydrogen finasteride iodide and a dihydrogen dutasteride iodide are oxidized by oxone for systhesis of finasteride and dutasteride, and the method has the characteristics that reaction operation is simple and convenient, raw materials are low in price and easy to obtain, and the yield and the purity are high. In particular, oxone is non-toxic, stable, easy to operate and more suitable for large-scale industrial production, and reagents which are harmful to the environment and high in price are avoided. The method can be further applied to forming of double bonds between the 1-position and the 2-position of an intermediate in other finasteride and dutasteride processes. The invention further provides a synthesis method of dihydrogen dutasteride; according to the method, a corresponding ester raw material has a one-pot reaction with 2,5-bis(trifluoromethyl)aniline under the activation of boron tribromide, and dihydrogen dutasteride with the yield of 93% is obtained.
TOPICAL COMPOSITIONS COMPRISING 5-ALPHA REDUCTASE INHIBITORS
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, (2010/03/31)
The present invention relates to topical compositions comprising 5α-reductase inhibitors. The present invention also includes processes for preparation of such topical compositions and methods of using them.