Mannich Base Derivatives of 1,2-Benzisothiazolin-3-one: Syntheses, Crystal Structures and Bioactivities

作者：Wang Xiang-Hui; Shao Yan -Dong; Wu Yuan-Yuan; Lin Qiang^*

来源：Chinese Journal of Structural Chemistry, 2014, 33(9): 1395-1400.

• 1,2-benzisothiazol-3(2H)-one
• syntheses
• crystal structure
• bioactivity

Twelve Mannich base derivatives of 1,2-benzisothiazolin-3-one were synthesized by the reaction of 1,2-benzisothiazol-3(2H)-one (BIT) with different amines and formaldehyde. All the compounds were characterized by elemental analysis, IR spectroscopy, MS and H-1 NMR. The crystal structure for 2,2'-methylenebis(benzo[d]isothiazol-3(2H)-one) (3) has been determined by X-ray single-crystal structure analysis. Compound 3 (C15H10N2O2S2) crystallizes in the monoclinic system, space group C2/c with a = 25.052(8), b = 4.510(1), c = 11.948(4) angstrom, beta = 100.992(4)degrees, V = 1325.2(7) angstrom(3), M-r = 314.37, D-c = 1.576 Mg.m(-3) mu = 0.25 mm(-1), F(000) = 648, Z = 4, R = 0.034 and wR = 0.087. The preliminary biological test indicated that the compounds (2b, 2c) showed growth inhibitory activity against the gram-positive and gram-negative bacteria.

• 出版日期2014
• 单位海南师范大学