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【结 构 式】 
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【药物名称】LF-16.0335 【化学名称】4-[4-[1-[2,4-Dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)phenylsulfonyl]pyrrolidin-2(S)-ylcarbonyl]piperazin-1-ylcarbonyl]benzamidine dihydrochloride 【CA登记号】202720-59-0, 202602-34-4 (free base) 【 分 子 式 】C35H38Cl4N6O5S 【 分 子 量 】796.60631 |
【开发单位】Fournier (Originator) 【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Antiallergy/Antiasthmatic Drugs, Asthma Therapy, Drugs for Allergic Rhinitis, Non-Opioid Analgesics, Pharmacological Tools, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders, Bradykinin B2 Antagonists, Non-Steroidal Antiinflammatory Drugs |
合成路线1
Title compound was obtained by coupling the sulfonylprolylpiperazine derivative (I) with 4-amidinobenzoic acid (II) in the presence of EDC and HOBt in DMF, followed by conversion to the dihydrochloride salt.
| 【1】 Dodey, P.; Bondoux, M.; Houziaux, P.; Barth, M.; Ou, K. (Laboratoires Fournier SA); N-Benzenesulphonyl-L-proline derivs. as bradykinin B2 agonists. EP 0925295; US 6071917; WO 9803503 . |