An improved and novel process for the synthesis of antiviral drug Darunavir using 4-(1,3-dioxoisoindolin-2-yl)benzene-1-sulphonyl chloride was described to eliminate the critical furan dimer impurity which will be formed during the process. The best reaction conditions were identified by evaluating the impurity profile and their formation during the synthesis. The optimization of the process was made to control the furan dimer impurity which was one of the critical parameters in the synthesis of darunavir. All the impurities formed during the synthesis were identified, synthesized and characterized.
An economical new process route has been developed for the
large-scale synthesis of memantine hydrochloride (1) an anti-Alzheimer's drug. The procedure involves the conversion of 1,3-dimethyl adamantane (2) to formamide intermediate 8 as a key
step, followed by hydrolysis to (1-amino-3,5-dimethyl adamantane) hydrochloride (1) in good yield.
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