Matrix metalloprotease inhibitors and synthetic method thereof
A technology of protease inhibitors and matrix metals, applied in the field of matrix metalloproteinase inhibitors and synthesis, to achieve the effects of short synthesis process routes, easy availability of raw materials, and low production costs
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[0025] Synthesis of benzenesulfonyl-D-alanine:
[0026]
[0027] Add 2.56ml (20mmol) of benzenesulfonyl chloride to 1.96g (22mmol) of D-alanine in Na 2 CO 3 solution (4.45gNa 2 CO 3 Dissolve in 30ml of water), under vigorous stirring, react at 70°C for 0.5hr. After the reaction was completed, cool in an ice bath, adjust the pH value to 2.5 with concentrated hydrochloric acid, put it in the refrigerator overnight, and precipitate a white precipitate, filter, wash the filter cake with a small amount of ice water, recrystallize with distilled water, and dry to obtain 1.58 g of the target product. : 34.5%, mp: 126-128°C, [α]=+32.2° (0.025g / ml methanol solution, room temperature) (R)-5-phenyl-N-((2-benzenesulfonamide)-1- Synthesis of oxy-propyl)-1,3,4-thiadiazol-2-amine
[0028]
[0029] Dissolve 1.37g (6mmol) benzenesulfonyl-D-alanine and 0.69g (6mmol) N-hydroxysuccinimide in dioxane, add DCC dioxane solution at room temperature, and react at room temperature for 4hr ,...
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