- Facile ring opening of 2,3-epoxy-steroids with aromatic amines in ionic liquids
-
Efficient ring opening of steroidal 2,3-epoxides with stoichiometric amount of aromatic amines has been carried out using an ionic liquid ([bmim]+[BF4]-) both as solvent and catalyst. The reactions were completely regio- a
- Horvath, Anita,Skoda-Foeldes, Rita,Maho, Sandor,Berente, Zoltan,Kollar, Laszlo
-
-
Read Online
- A new and efficient method for the synthesis of rocuronium bromide
-
Rocuronium bromide has been used as an aminosteroid non-depolarizing neuromuscular blocker and muscle relaxant. In this work, a new and efficient route for preparing a key intermediate 2β-(4-morpholinyl)-16β-(1-pyrrolidinyl)-5α-androstan-3α,17β-diol (6) was developed through a ring-opening of epoxide followed by introducing and pyrrolidine. Compound 6 can easily provide rocuronium bromide and the overall yield of compound 6 in 5 steps increased to 57.8%, which was higher than currently reported methods. Extraordinarily, this method would avoid the generation of disubstituted impurities E and F which are difficult to remove.
- Wu, Xue-Ying,Wang, Yao-Ling,Hai, Li,Gong, Ping,Wu, Yong
-
p. 487 - 492
(2017/01/28)
-
- Novel method for preparing rocuronium bromide
-
The invention relates to a novel method for preparing rocuronium bromide 1-[17beta-acetoxyl-3alpha-hydroxyl-2beta-(4-morpholinyl)-androstane-16beta-yl]-1-(2-propenyl) pyrrole bromide, the problem of chemoselectivity of pyrrolidine open epoxy in an original line is solved, generation of byproducts is avoided, reaction yield is greatly improved, the production cost is reduced, column chromatography separation is avoided, and aftertreatment purification is implemented easily.
- -
-
Paragraph 0013
(2017/11/18)
-
- A facile and general synthesis of 2β-aminosteroids
-
A facile and general synthesis of 2β-aminosteroids in high yields from 2,3α-epoxy-5α-androstan-17-one by regioselective aminolysis is developed using a zinc chloride/water catalytic system. The reaction is successful with both aliphatic and aromatic amine
- Ke, Xianbing,Hu, Hao,Zhou, Dingshan,Xu, Wenjin,Zhu, Qifeng,Reddy, Nimmanapalli Pulla,Hu, Xianming
-
experimental part
p. 1255 - 1260
(2009/12/07)
-