- A 3-carbonyl-4-aza-5-androstene -17 β method for preparing derivatives of
-
The invention provides a preparation method of a 3-carbonyl-4-aza-5-androstene-17beta derivative. The preparation method comprises the following steps: suspending an A-nor-3,5-cracking-androstan-5-keto-3-carboxylic acid-17beta derivative II in an aqueous solution of ammonium acetate for performing a ring-closure reaction; cooling a reaction product; adjusting the PH value of the reaction product by using industrial ammonia water; filtering the reaction product by spinning; drying the reaction product by spinning; and washing a filter cake by using water, and drying the filter cake to obtain a 3-carbonyl-4-aza-5-androstene-17beta derivative I, wherein R in a formula II and a formula I is carbonyl, carboxylic acid, carboxylic ester, amide, acetyl, hydroxyl, alkyl, ether or chloro. The preparation method has the advantages of mild reaction condition in the absence of inorganic solvents, low requirements on equipment and pre-treatment, complete reaction, and high product purity of over 99 percent without purification; moreover, a spinning-filtered mother solution is recovered, so that the emission of three wastes is reduced greatly; in the whole reaction, used raw materials are readily available; and meanwhile, the reaction yield is high, and the preparation method is economical and environmentally friendly, and is convenient for industrial implementation.
- -
-
Paragraph 0028; 0029; 0030; 0036; 0037
(2016/10/31)
-
- DECAHYDRO-1H-INDENOQUINOLINONE AND DECAHYDRO-3H-CYCLOPENTAPHENANTHRIDINONE CYP17 INHIBITORS
-
Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
- -
-
Page/Page column 43
(2010/05/13)
-
- A microwave promoted and Lewis acid catalysed solventless approach to 4-azasteroids
-
The preparation of 3-oxo-4-azasteroid from A-nor-3,5-secosteroid-3-oic acid is described in a solventless condition catalysed by Lewis acid under microwave irradiation. We utilized urea as an environmentally benign source for the generation of ammonia for the aza cyclization reaction.
- Borthakur, Moyurima,Boruah, Romesh C.
-
p. 637 - 641
(2008/09/19)
-
- New approach to 3-oxo-4-aza-5α-androst-1-ene-17β-(N-tert- butylcarboxamide)
-
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.
- Jiang, Zhong-Xing,Ye, Jing-Quan,Jiang, Li,Zhao, Ying-Sheng
-
p. 690 - 693
(2007/10/03)
-
- 4-aza steroids
-
The invention related to 4-aza-17β-(cyclopropoxy)-androst-5α-androstan-3-one, 4-aza-17β-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20lyase, 5α-reductase and C17α-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formula:
- -
-
-
- 17-BETA-CYCLOPROPYL(AMINO/OXY) 4-AZA STEROIDS AS ACTIVE INHIBITORS OF TESTOSTERONE 5-ALPHA-REDUCTASE AND C17-20-LYASE
-
The invention related to 4-aza-17 beta -(cyclopropoxy)-androst-5 alpha -androstan-3-one, 4-aza-17 beta -(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5 alpha -reductase and C17 alpha -hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have general formula (I).
- -
-
-