73.
    发明专利
    失效

    公开(公告)号:JPH05239002A

    公开(公告)日:1993-09-17

    申请号:JP7558892

    申请日:1992-02-27

    摘要: PURPOSE:To obtain a new tricyclic compound useful as an anti-histamine agent and an antiallergic agent having low side effects and excellent selectivity. CONSTITUTION:A tricyclic compound of formula I [X is CH=CH, CH2O, CH2CH2 or O; Y is CO or CH(OH); R is lower alkyl; R is H or lower alkyl] and its pharmaceutically permissible salt such as ethyl 4[N-[3-(10,11-dihydro-5H- dibenzo[a,d] cyclohepten-5-ylidene)propyl]-N-methylaminolacetacetate. The compound is obtained by reacting a compound of formula II with a compound of formula III (Z is halogen) in a solventless state or in a solvent in the presence or absence of a base (dehydrohalogenating agent) and optionally hydrolyzing with an acid or a base in a solvent. A daily dose of the compound to a patient is usually 1-500mg per adult in the case of oral administration and properly increased or decreased depending upon age, symptom, etc.

    PRODUCTION OF PHENYLPROPIONIC ACID DERIVATIVE

    公开(公告)号:JPH02292244A

    公开(公告)日:1990-12-03

    申请号:JP11327689

    申请日:1989-05-02

    摘要: PURPOSE:To obtain a free acid by treating methyl 3-[p-(trans-4- aminomethylcyclohexylcarbonyl)phenyl]propionate hydrochloride, etc., in the presence of a fungus, etc., belonging to the genus Aspergillus or Mucor. CONSTITUTION:A compound expressed by the formula (R is benzyl, phenyl, lower alkyl, etc.) or salt thereof is treated in the presence of microbial cells of a microorganism selected from fungi belonging to the genus Aspergillus or Mucor, yeasts belonging to the genus Candida, etc., bacteria belonging to the genus Pseudomonas, etc., and actinomyces, and obtained culture or extract thereof to afford a free acid of the compound expressed by the formula and salt thereof. The abovementioned reaction is carried out in water or a suitable buffer solution at 25 to 35 deg.C for 10 to 15hr while being kept at pH4 to 7. The resultant compound is produced in high purity and yield under mild conditions according to the aforementioned reaction without causing side reaction. The abovementioned method is excellent in safety and simple post-treatment.