Some common heterocyclic compound, 112101-81-2, name is R-5-(2-Aminopropyl)-2-methoxybenzenesulfonamide, molecular formula is C10H16N2O3S, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Safety of R-5-(2-Aminopropyl)-2-methoxybenzenesulfonamide
EXAMPLES Example 1 Preparation of (R)-2-bromo-N- [2- (4-methoxy-3-aminosulfonyl-phenyl)-1-methyl-ethyl] – acetamide) 1.0 g of (R)-2- (4-methoxyphenyl-3-aminosulfonyl-phenyl)-1-methylethylamine was dissolved in 50 ml of methylene chloride. 0.72 g (2.0 eq) of triethyamine was added to the resultant solution and cooled to 0 to 5C. Then, 1.44 g (2.0 eq) of bromoacetyl bromide was added dropwise to the resultant solution and stirred at 0 to 5C. After it was confirmed by HPLC that the starting materials were completely consumed, 100 ml of ethyl acetate and then 50 ml of 10% HCI were added to the resultant solution and stirred. The ethyl acetate layer was separated and washed with 50 ml of a 10% K2CO3 solution and dried over MgS04, and then, filtered and concentrated. The obtained concentrate was dissolved in ethyl acetate and recrystallized with hexane to obtain the title compound (1.2 g). Yield : 80.0% NMR (DMSO-d6) : 1.15 (3H, d), 2. 6-2. 8 (2H, m), 3.8 (2H, s), 3.90 (4H, s), 7.0 (2H, s), 7.1 (1H, d), 7.4 (1H, d), 7.6 (1H, d), 8.21 (2H, d). [a] 24D = + 5.0 (C=1, MeOH)
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 112101-81-2, its application will become more common.
Reference:
Patent; CJ CORPORATION; WO2005/56521; (2005); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics