Improvements in or relating to method of preparing 1-substituted-3-pyrrolidylmethyl benzilates and the salts thereof, and the compounds resulting from said method
Реферат: The invention comprises pyrrolidylmethyl benzilates of the general formula: <FORM:0799032/IV (b)/1> wherein R is an alkyl, alkenyl, aryl or aralkyl group, and acid addition and quaternary salts of these compounds; it also comprises a process for the preparation of compounds of the above general formula by esterifying a 1-substituted-3-pyrrolidylmethyl alcohol with benzilic acid, or with a benzilic acid ester by ester interchange. In an example, methyl benzilate is refluxed in n-heptane with 1-methyl-3-pyrrolidylmethyl alcohol, in the presence of metallic sodium, in a Dean and Stark apparatus to give 1-methyl-3-pyrrolidylmethyl benzilate which is subsequently converted to the hydrochloride. Other 1 - substituted - 3 - pyrrolidylmethyl benzilates of the above general formula which are prepared according to the invention include those wherein R is an ethyl, n-propyl, isopropyl, allyl, butyl and benzyl group. Suitable acid addition salts include the hydrohalides, sulphates, phosphates, maleates, acetates, citrates, succinates and tartrates. Suitable quaternary salts include those obtained by addition of a methyl halide, sulphate, benzenesulphonate or p-toluenesulphonate or an ethyl, propyl or benzyl halide. The products are used pharmaceutically as antispasmodics. Specification 799,030 is referred to.
Method of producing enamines
Номер патента: RU2586046C2. Автор: Дуглас К. БЛЭНД,Тодд Уилльям ТОЙЗЕН. Владелец: ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи. Дата публикации: 2016-06-10.