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. name: R-5-(2-Aminopropyl)-2-methoxybenzenesulfonamide
EXAMPLE 34 R-(-)-5-[2-[2-(5-Fluoro-2-methoxyphenoxy)-ethylamino]propyl]-2-methoxybenzenesulfonamide hydrochloride A suspension of 1.00 g of R-(-)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide [[alpha]D25 -13.8 (C=1,MeOH), m.p.156.5-160.5 C. (H2 O) ] 11.00 g of 2-(2-bromoethoxy)-4-fluoroanisole and 0.20 g of potassium iodide in 40 ml of N,N-dimethylformamide was heated for 10 hours at 85 C. After cooling, the reaction mixture was poured into water, made alkaline with 10% sodium hydroxide aqueous solution and extracted with ethyl acetate. The extract was washed with water, dried and evaporated. The residue was chromatographed on silica gel using chloroform-methanol (9:1) as an eluant to give 0.81 g of the free base as colorless crystals which were recrystallized from methanol as colorless needles, m.p.144-145 C. Analysis for C19 H25 FN2 O5 S: Calculated %: C, 55.33; H, 6.11; N, 6.79. Found %: C, 55.20; H, 5.93; N, 6.54.
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; Hokuriku Pharmaceutical Co., Ltd.; US4971990; (1990); A;,
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