14805-29-9, exo-Hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated
Example 2To the reaction mixture containing Compound (C) which was obtained in the above Example 1 were added (3aR,4S,7R,7aS)-hexahydro-4,7-methano-2H-isoindole-1,3-dione [Compound (D)] (22.6 g, 136.8 mmol), potassium carbonate (15.1 g, 109.3 mmol) and toluene (44 g).Then, the toluene (44 g) was distilled out from the mixture, water (0.82 g) was added thereto, and the resulting mixture was reacted under reflux for 8 hours.Then, the reaction mixture was cooled to room temperature, and water (400 g) was added to the mixture.The mixture was separated with a separating funnel, and the toluene layer was washed with 2.3percent (W/W) brine (350 g).Further, active carbon (1.8 g) was added to the toluene solution, and the mixture was stirred for 1 hour.The active carbon was removed by filtration to give a toluene solution containing (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl) piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione (2-[[(1R,2R)-2-[[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]-methyl]hexahydro-(3aS,4R,7S,7aR)-4,7-methano-1H-isoindole-1,3(2H)-dione) [Compound (E)] (341.4 g).The yield of Compound E was 94.3percent The yield of Compound (E) was calculated based on the analytical result that the content of the compound in the toluene solution was 12.4percent (w/w) (which was calculated by LC absolute calibration curve method).And, the production rate of by-product (R) was 0.013percent (which was calculated with the following formula (a))., 14805-29-9
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Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; US2011/263848; (2011); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles