Pennem derivates containing formamide heterocycle sulfonic acid amide sulfhydryl pyrrolidine
A sulfonylamino, methyl group technology, applied in the field of medicine, can solve the problems of poor antibacterial effect, long elimination half-life and the like
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Embodiment 1
[0099] Example 1 (2S, 4S)-4-mercapto-2-formyl [(2-sulfonylamino-pyridin-6-yl) amino] -1- (tert-butoxycarbonyl) pyrrolidine preparation
[0100]Add (2S,4S)-4-acetylthio-2-carboxy-1-(tert-butoxycarbonyl)pyrrolidine 7.8g (27mmol) into the dry reaction flask, anhydrous tetrahydrofuran 100ml, under nitrogen protection, in Add 6.5g (40mmol) of 1,1-carbonyldiimidazole (CDI) at room temperature, react for 0.5h, add 8.7g of 6-aminopyridine-2-sulfonamide in tetrahydrofuran (50mmol / 100ml) below 0°C, and continue the reaction for 0.5 h, then add 40ml of 1mol / L hydrochloric acid dropwise, extract with ethyl acetate (50ml×2), wash the organic phase with water and saturated sodium chloride solution successively, concentrate under reduced pressure, add 100ml of 3mol / L hydrochloric acid to the residue, and stir for 2h , adjusted to basicity with a dilute alkaline solution, and a solid was precipitated, which was recrystallized from a mixed solution of ethyl acetate-cyclohexane (5:1) to obt...
Embodiment 2
[0101] Example 2 (2S, 4S) -4-mercapto-2-formyl [(4-sulfonylamino-thiazol-2-yl) amino] -1- (tert-butoxycarbonyl) pyrrolidine preparation
[0102] Refer to Example 1 for specific operations, throw (2S, 4S)-4-acetylthio-2-carboxy-1-(tert-butoxycarbonyl)pyrrolidine 7.8g (27mmol), 2-aminothiazole-4-sulfonamide 9g (50mmol) to obtain 8.9g of (2S, 4S)-4-mercapto-2-formyl[(4-sulfonylamino-thiazol-2-yl)amino]-1-(tert-butoxycarbonyl)pyrrolidine, Yield: 81.2%.
Embodiment 3
[0103] Example 3 (2S, 4S)-4-mercapto-2-formyl [(4-sulfonylamino-oxazol-2-yl) amino] -1- (tert-butoxycarbonyl) pyrrolidine preparation
[0104] Refer to Example 1 for specific operations, throw (2S, 4S)-4-acetylthio-2-carboxy-1-(tert-butoxycarbonyl)pyrrolidine 7.8g (27mmol), 2-aminooxazole-4-sulfonyl Ammonia 8.2g (50mmol), to get (2S,4S)-4-mercapto-2-formyl[(4-sulfonylamino-oxazol-2-yl)amino]-1-(tert-butoxycarbonyl)pyrrolidine 8.4 g, yield: 78.9%.
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