| 摘要 |
PROBLEM TO BE SOLVED: To simply and inexpensively obtain a 2,3-dihydrobenzofuran derivative useful as an antianxiety agent, etc., in high purity and yield and fewer steps by reacting a specific compound with a specific compound. SOLUTION: A compound of formula I [(X) is a leaving group; * is an asymmetric carbon] is reacted with a compound of the formula: H2N-(CH2)n-A-B [(n) is 2-6; A is HNCO or HNSO2; B is naphthyl, thienyl, pyridyl, etc.], and as necessary, a lower alkyl is introduced into NH2 group of reaction product by an alkylating agent or the compound of formula I is reacted with a compound of formula II (R1 is H or a lower alkyl) to provide the objective 2,3- dihydrobenzofuran derivative (salt) represented by formula III, e.g. (R)-2-(N-(4- benzoylamino)butyl)aminomethyl-2,3-dihydrobenzo[b]furan hydrochloride. Furthermore, it is preferable to react the compound of formula I with a compound of the formula: H2N-(CH2)n-A-B [(n) is 4; A is HNCO; B is phenyl]. |
