| 摘要 |
<p>PURPOSE: To obtain the subject new compound presenting high affinity for serotonin1 A receptors, thus useful as a medicine for treating serotonin nervous system-related diseases such as an anxiolytic agent, antidepressant, eating disorder-remedying agent, hypotensive agent or antiemetic agent. CONSTITUTION: This new compound, a 2,3-dihydrobenzofuran derivative, is expressed by formula I (R<1> is H or a lower alkyl; R<2> is naphthyl, pyridyl, furyl or thienyl; (n) is 2-6; A is carbonyl or sulfonyl; * denotes an asymmetric carbon atom), e.g. 2- N-[4-(1-naphthoylamino) butyl]}aminomethyl-2,3- dihydrobenzo[b]furan. The compound of formula I is obtained by subjecting a compound of formula II (R<11> is an amino-protecting group or lower alkyl) and a compound of formula X-A-R<2> (X is an eliminable atom or group) to amidation in a solvent (e.g. chloroform) pref. in the presence of a base (e.g. sodium bicarbonate) at -25 to 5 deg.C followed by, where needed, elimination of the protecting group.</p> |
