- Etiprednol dicloacetate, a new soft glucocorticoid drug candidate. Development of chemistry
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During development of chemistry of the soft drug candidate etiprednol dicloacetate (BNP-166) 1) optimization studies on the three-step chemical synthesis resulted in a process that could be scaled-up to the kg level, 2) the impurity profile was determined, 3) synthetic routes were developed for the preparation of the radiolabeled target compound, and 4) a series of hydroxylated metabolites was prepared.
- Csanadi,Horvath,Szekeres,Hasko,Ila,Ivanics,Patthy,Salat,Seres,Pallagi,Toth,Szederkenyi,Konya,Tegdes,Bodor,Zubovics, Zoltan
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p. 349 - 359
(2007/10/03)
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- Synthesis of N-substituted 3-oxo-17β -carboxamide-4-aza-5α-androstanes and the tautomerism of 3-oxo-4-aza-5-androstenes
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An N-aryl-3-oxo-4-aza-5α -androst-1-ene-17β carboxamide and three N-aryl or alkyl substituted 17α -hydroxy-3-oxo-4-aza-5α -androstane-17β -carboxamides were synthesized as antiandrogen candidates from 3-oxoandrost-4-ene-17β - carboxylic acid and androst-4-ene-3,17-dione respectively. The chemo- and stereoselective reduction of 3-oxo-4-aza-5-ene intermediates with formic acid and their tautomerism in a solution of chloroform and methanol were described.
- Xia, Peng,Yang, Zheng-Yu,Xia, Yi,Zhang, Hao-Bing,Zhang, Ke-Hua,Sun, Xun,Chen, Ying,Zheng, Yun-Qing
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p. 703 - 716
(2007/10/03)
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- Amines useful in producing pharmaceutically active CNS compounds
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Disclosed are Δ9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17(20) -steroids (Va and Vb) and Δ9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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