With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.87691-88-1,3-Piperazinobenzisothiazole hydrochloride,as a common compound, the synthetic route is as follows.
N- [4- (2-CHLORO-ETHYL)-2-METHYL-PHENYL]-N-METHYL-ACETAMIDE (0.300 g, 1. 153 mmol), 3-PIPERAZIN-1-YL-BENZO [d] isothiazole hydrochloride (0.442 g, 1.729 MMOL), potassium carbonate (0.237 g, 1.729 MMOL), and potassium iodide (0.173 g, 1.153 MMOL) in ACETONITRILE (3.5 mL) was subjected to 150 C for 30 min. under microwave assistance using a Smith Personal Chemistry microwave. The reaction was diluted with H20 (50 mL) and CH2CI2 (100 mL). The layers were separated and the organics washed with 1 N HCI (2x 25 mL). The aqueous layer was made basic and extracted with CH2CI2 (3X50 mL). The organics were dried (MGS04), and concentrated to a solid residue. The residue was subjected to chromatography (MEOH : CH2CI2 1 : 19) and collected as an amorphous residue and taken up in 1,4-dioxane and subjected to HCI gas for 10 min. The resulting solid was collected by filtration and dried at 50 C under high vacuum overnight (0.770 g). 100% purity at 254nm; LCMS (APCI) : 409.2 [M+H] +.
The synthetic route of 87691-88-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/41793; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com