アルノロール 化学特性,用途語,生産方法
Originator
Arnolol,ZYF Pharm Chemical
Manufacturing Process
2 methods of producing of 1-[4-(2-methoxyethyl)-phenoxy]-3-amino-3-
methyl-butan-2-ol:
1). 19.0 g of 1-[4-(2-methoxyethyl)phenoxy]-3-nitro-3-methylbutan-2-ol are
hydrogenated at 60°C and under a pressure of 6 bar in a mixture of 250 ml of
ethanol and 50 ml of glacial acetic acid in the presence of 4.0 g of palladiumon-
charcoal (10% Pd). After the mixture has been filtered and the solvent has
been evaporated off, the residue is rendered alkaline with 2 N NaOH and the mixture is extracted with CH2Cl2. The organic phase is washed with water and
dried with Na2SO4 to give, after evaporation, 15.0 g of the 1-[4-(2-
methoxyethyl)phenoxy]-3-amino-3-methylbutan-2-ol, melting point 120°-
122°C (dec.).
2). 18.3 g of zinc dust are gradually added to 20.0 g of 1-[4-(2-methoxyethyl)
phenoxy]-3-nitro-3-methylbutan-2-ol in 400 ml of ethanol and 60 ml of
concentrated hydrochloric acid at 50°-60°C. The mixture is stirred at this
temperature for 1 h and filtered and the solvent is evaporated off. After 200
ml of 40% strength NaOH have been added, the product is extracted with
methylene chloride. Solvent is distilled and the 1-[4-(2-methoxyethyl)
phenoxy]-3-amino-3-methylbutan-2-ol is produced, melting point 120°-122°C
(dec.).
Therapeutic Function
Beta-adrenergic blocker (ophthalmic)
アルノロール 上流と下流の製品情報
原材料
準備製品