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    • 1. 发明申请
    • Process for producing 1,2,4-triazole compound and intermediate therefor
    • 生产1,2,4-三唑化合物及其中间体的方法
    • US20060189811A1
    • 2006-08-24
    • US10565678
    • 2004-07-23
    • Hiroshi NakamuraJunichiro UdaAtsushi OhnoTakahiro Sato
    • Hiroshi NakamuraJunichiro UdaAtsushi OhnoTakahiro Sato
    • C07D403/14
    • C07D403/14
    • Provided is a process for producing 1,2,4-triazole compound (5), or a salt or hydrate thereof which comprises reacting compound (1) with Rc-X (2) to give compound (3), reacting compound (3) with a nitrilization agent to give compound (4), and then removing the group Rc, as shown by the reaction scheme: (Wherein Ra, Rb and Rd represent a group, Rc represents a group which can be removed by an acid) A 1,2,4-triazole compound (5) having an optionally substituted 2-cyanopyridin-4-yl group at 3-position and an optionally substituted aromatic group at 5-position which inhibits a xanthine oxidase and is useful for treatment of gout and hyperuricemia can be obtained from compound (1) in a high yield without requiring isolation of reaction products in the course of reactions.
    • 本发明提供了使化合物(1)与Rc-X(2)反应得到化合物(3),使化合物(3)与化合物(3)反应的1,2,4-三唑化合物(5)或其盐或水合物的方法, 与硝化剂反应得到化合物(4),然后除去Rc基团,如反应方案所示:(其中Ra,Rb和Rd表示基团,Rc表示可被酸除去的基团)A 1 ,3位具有任选取代的2-氰基吡啶-4-基的2,4-三唑化合物(5)和5位上任意取代的芳族基团,其抑制黄嘌呤氧化酶并且可用于治疗痛风和高尿酸血症 可以以高产率从化合物(1)获得,而不需要在反应过程中分离反应产物。
    • 4. 发明申请
    • Benzoxepino-11-piperidylidene compounds and process for production thereof
    • 苯并恶灵-11-哌啶基化合物及其制备方法
    • US20060217556A1
    • 2006-09-28
    • US10553034
    • 2004-04-14
    • Junichiro UdaTomomitsu SasakiTakahiro SatoTsutomu Inoue
    • Junichiro UdaTomomitsu SasakiTakahiro SatoTsutomu Inoue
    • A61K31/4741C07D491/02
    • C07D491/04A61K31/553
    • Provided are a process for producing an acid addition salt of a 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid alkyl ester by reacting a 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid alkyl ester with an acid, and a process for producing 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid using the acid addition salt as an intermediate. By using as an intermediate an acid addition salt of a 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid alkyl ester to produce 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid, the metals used in the synthetic reaction steps and the organic compounds mainly by-produced during production are readily separated from a reaction liquid by a simple procedure, and the by-products are sufficiently removed without using a purification step by chromatography, thereby enabling mass production and enhancing production efficiency.
    • 提供了制备3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸烷基酯的酸加成盐的方法 通过使3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸烷基酯与酸反应, 使用酸加成盐作为中间体的3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸。 通过使用3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸烷基酯的酸加成盐 制备3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶]亚基)哌啶子基]丙酸,合成反应步骤中使用的金属和有机化合物 主要通过简单的方法容易地从生产中副产的副产物与反应液分离,并且副产物被充分除去,而不需要通过色谱法的纯化步骤,从而可以批量生产并提高生产效率。