| 摘要 |
PROBLEM TO BE SOLVED: To industrially and advantageously produce a bi- and hetero-cyclic compound useful as an intermediate for producing antibiotic substances by using a readily available optically active compound as a raw material. SOLUTION: A compound of formula I [R<1> is H, a (substituted)arylmethyl or a 1-6C alkyl; X is a halogen] and a compound of the formula, R<2> -OH (R<2> is a 1-6C alkyl) are treated in the presence of a hydrogen chloride and converted into a compound of formula II, which is then reacted with a compound of formula III (R<3> is H or a 1-6C alkyl; R<4> and R<5> are each a 1-6C alkyl). The resultant compound is subsequently cyclized. The prepared cyclized compound is then reacted with a compound of the formula, R<6> -SO3 H [R<6> is a 1-6C alkyl or a (substituted)aryl] and subsequently reacted with a metallic salt of a compound of the formula, R<7> -COSH (R<7> is same as R<6> ) to afford a thioalcohol derivative. A protecting group of the resultant derivative is then eliminated to provide the objective compound of formula IV, e.g. (6S)-6-mercarpto-6,7-dihydro-5H- pyrrolo[1,2-a]imidazole. |
