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    • 3. 发明授权
    • 5-치환된 인돌 유도체의 제조방법
    • 5-치환된인돌유도체의제조방법
    • KR100411599B1
    • 2003-12-18
    • KR1020010065508
    • 2001-10-23
    • 동방에프티엘 주식회사
    • 김영배이정권최선희강문석
    • C07D209/14
    • PURPOSE: A process for preparing 5-substituted indol derivative is provided, thereby the 5-substituted indol derivative can be prepared in higher yield because a process for preparing an intermediate, ethyl 5-substituted indol-2-carboxylic acid is not required. CONSTITUTION: A process for preparing 5-substituted indol derivative comprises the steps of: treating p-substituted aniline derivative of formula(II) with sodium nitrate and hydrochloric acid to prepare p-substituted azoate chloride; reacting the p-substituted azoate chloride with ethyl alpha-methyl acetoacetate to prepare azoester; treating the azoester with hydrochloric acid and methanol to prepare ethyl pyruvate p-substituted phenylhydrazone; reacting the pyruvate p-substituted phenylhydrazone with polyphosphoric acid in toluene to prepare 5-substituted indol-2-carboxylate; and reacting the ethyl 5-substituted indol-2-carboxylate with a mixture of sulfuric acid and acetic acid or hydrogen bromide, wherein R is methyl, bromo, cyano, carboxy and methoxy.
    • 目的:提供一种制备5-取代的吲哚衍生物的方法,因此可以以较高的收率制备5-取代的吲哚衍生物,因为不需要制备中间体5-取代的吲哚-2-羧酸的方法。 构成:制备5-取代的吲哚衍生物的方法包括以下步骤:用硝酸钠和盐酸处理式(II)的对位取代的苯胺衍生物以制备对取代的偶氮酸氯化物; 使对位取代的偶氮酸氯与乙基α-甲基乙酰乙酸酯反应制备偶氮酯; 用盐酸和甲醇处理该偶氮酯以制备丙酮酸乙酯对取代的苯腙; 使丙酮酸对位取代的苯腙与多磷酸在甲苯中反应以制备5-取代的吲哚-2-羧酸酯; 使5-取代的吲哚-2-羧酸乙酯与硫酸和乙酸或溴化氢的混合物反应,其中R是甲基,溴,氰基,羧基和甲氧基。
    • 4. 发明公开
    • 구굴스테론의 제조방법
    • 生产防腐剂的方法
    • KR1020030033504A
    • 2003-05-01
    • KR1020010065507
    • 2001-10-23
    • 동방에프티엘 주식회사
    • 김영배이정권최선희강문석
    • C07J13/00
    • C07J13/007A61K31/56
    • PURPOSE: Provided are Z- and E-type guggulsterone, which inhibits subcutaneous fat and has anti-fatness and cholesterol inhibiting activities and are produced from 16-dihydro pregnaron acetate. CONSTITUTION: The Z- and E-type guggulsterone(formula 2a and 2b) having the ratio of 80:20 are produced by a process comprising the steps of: reducing the 16-dihydro pregnaron acetate in an organic solvent by Red-Aldrich to prepare 5,16-pregnadiene-3beta-20 diol, wherein the organic solvent is toluene, xylene, cumene, or methyl ethyl ketone; oxidizing the 5,16-pregnadiene-3beta-20 diol by p-toluene sulfonic acid to prepare a mixture of 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diacetate; dissolving the mixture of 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diacetate in methanol solution in which potassium hydroxide is dissolved and refluxing to obtain 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diol; oxidizing the 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diol by NiO in the presence of a hydrogen acceptor mixture of cyclopentanone and acetone.
    • 目的:提供Z型和E型古格斯酮,其抑制皮下脂肪并具有抗脂肪和胆固醇抑制活性,并由16-二氢孕烯乙酸酯制备。 构成:通过包括以下步骤的方法产生具有80:20比例的Z型和E型格格酮(式2a和2b),该方法包括:通过Red-Aldrich在有机溶剂中还原16-二氢孕烯乙酸酯以制备 5,16-孕二烯-3β-20二醇,其中有机溶剂是甲苯,二甲苯,异丙基苯或甲基乙基酮; 通过对甲苯磺酸氧化5,16-孕二烯-3β-20二醇以制备5,17(20) - 反式孕二烯-3β,16beta和3β,16α二乙酸酯的混合物; 将5,17(20) - 反式孕二烯-3βeta,16beta和3β,16α二乙酸酯的混合物溶解在其中溶解氢氧化钾并回流的甲醇溶液中,得到5,17(20) - 反式孕二烯-3βeta,16beta和3β ,16α二醇; 在环戊酮和丙酮的氢受体混合物存在下,通过NiO氧化5,17(20) - 反式孕二烯-3β,16beta和3β,16α二醇。
    • 6. 发明公开
    • 프로필벤질릭산 에스터로부터 염산 프로피베린의 제조방법
    • 用于制备作为中间体的O-N-丙氧基酸的丙酸氯丙酯的方法
    • KR1020050011139A
    • 2005-01-29
    • KR1020030050112
    • 2003-07-22
    • 동방에프티엘 주식회사
    • 박찬신이정권최선희
    • C07D211/44
    • PURPOSE: A process for preparing propiverine hydrochloride from O-n-propylbenzylic acid is provided, thereby easily preparing propiverine hydrochloride which has improved anti-choline and calcium-antagonizing activity and is useful for prevention and treatment of various urination disorders of domestic animals using O-n-propylbenzylic acid as an intermediate. CONSTITUTION: The process for preparing propiverine hydrochloride from O-n-propylbenzylic acid comprises the steps of: reacting O-n-propylbenzylic acid ester with 4-hydroxy-1-methylpiperidine to prepare propiverine; and crystallizing the propiverine with hydrochloric acid gas, wherein the O-n-propylbenzylic acid ester is prepared by reacting benzylic acid with one or more alcohols selected from methanol, ethanol, n-propanol and isopropanol to prepare benzylic acid ester, sequentially adding tetrahydrofuran, triphenylphosphine and 1-propanol into the benzylic acid ester under nitrogen condition, adding 40% diethylazodicarboxylate into the mixed solution, adding benzylic acid ester in tetrahydrofuran into the mixed solution and reacting them.
    • 目的:提供从丙基苄基酸制备盐酸丙酸的方法,从而容易地制备具有改善的抗胆碱和钙拮抗活性的丙酸炔丙酯,并且可用于预防和治疗使用基于丙基苄基的家畜的各种排尿障碍 酸作为中间体。 构成:从O-正丙基苄基酸制备盐酸丙酸的方法包括以下步骤:使O-正丙基苄基酯与4-羟基-1-甲基哌啶反应制备丙酸; 并用盐酸气体结晶丙酰胺,其中通过苄基酸与选自甲醇,乙醇,正丙醇和异丙醇的一种或多种醇反应制备苄酸酯,依次加入四氢呋喃,三苯基膦和 在氮气条件下将1-丙醇加入苄酸酯中,加入40%二乙基偶氮二羧酸二乙酯于混合溶液中,将苄酸酯在四氢呋喃中加入到混合溶液中并使其反应。
    • 7. 发明公开
    • 염산 프로피베린의 제조방법
    • 使用O-N-丙烯酸作为中间体制备丙酸盐酸盐的方法
    • KR1020050011138A
    • 2005-01-29
    • KR1020030050111
    • 2003-07-22
    • 동방에프티엘 주식회사
    • 박찬신이정권최선희
    • C07D211/44
    • PURPOSE: A process for preparing propiverine hydrochloride is provided, thereby easily preparing propiverine hydrochloride which has improved anti-choline and calcium-antagonizing activity and is useful for prevention and treatment of various urination disorders of domestic animals using O-n-propylbenzylic acid as an intermediate. CONSTITUTION: The process for preparing propiverine hydrochloride comprises the steps of: preparing O-n-propylbenzylic acid from benzylic acid by oxidizing benzylic acid with phosphate pentachloride and reacting the oxidized benzyl with 1-propanol, or by reacting benzylic acid with propylchloride; reacting the O-n-propylbenzylic acid with 4-hydroxy-1-methylpiperidine to prepare propiverine; and adding hydrochloric acid into propiverine to prepare propiverine hydrochloride.
    • 目的:提供一种制备盐酸丙酸的方法,从而易于制备具有改善的抗胆碱和钙拮抗活性的盐酸丙酸盐,并且可用于使用O-正丙基苄基酸作为中间体预防和治疗家畜的各种排尿障碍。 构成:盐酸丙酸盐的制备方法包括以下步骤:通过用五氯化磷与苄基酸氧化苄基酸,并将氧化的苄基与1-丙醇反应,或通过苄基酸与丙基氯反应,由苄酸制备O-正丙基苄基酸; 使O-正丙基苄基酸与4-羟基-1-甲基哌啶反应以制备丙酸; 并加入盐酸以制备盐酸丙酸。
    • 10. 发明公开
    • 5-치환된 인돌 유도체의 제조방법
    • 制备5代中性衍生物的方法
    • KR1020030033505A
    • 2003-05-01
    • KR1020010065508
    • 2001-10-23
    • 동방에프티엘 주식회사
    • 김영배이정권최선희강문석
    • C07D209/14
    • PURPOSE: A process for preparing 5-substituted indol derivative is provided, thereby the 5-substituted indol derivative can be prepared in higher yield because a process for preparing an intermediate, ethyl 5-substituted indol-2-carboxylic acid is not required. CONSTITUTION: A process for preparing 5-substituted indol derivative comprises the steps of: treating p-substituted aniline derivative of formula(II) with sodium nitrate and hydrochloric acid to prepare p-substituted azoate chloride; reacting the p-substituted azoate chloride with ethyl alpha-methyl acetoacetate to prepare azoester; treating the azoester with hydrochloric acid and methanol to prepare ethyl pyruvate p-substituted phenylhydrazone; reacting the pyruvate p-substituted phenylhydrazone with polyphosphoric acid in toluene to prepare 5-substituted indol-2-carboxylate; and reacting the ethyl 5-substituted indol-2-carboxylate with a mixture of sulfuric acid and acetic acid or hydrogen bromide, wherein R is methyl, bromo, cyano, carboxy and methoxy.
    • 目的:提供5-取代的吲哚衍生物的制备方法,因为5-取代的吲哚衍生物可以以更高的收率制备,因为不需要制备中间体5-取代的吲哚-2-羧酸乙酯的方法。 构成:制备5-取代的吲哚衍生物的方法包括以下步骤:用硝酸钠和盐酸处理式(II)的对取代苯胺衍生物以制备对取代的偶氮氯化物; 使对取代的偶氮氯化物与乙酰乙酸乙酯乙酯反应,制备亚硒酯; 用盐酸和甲醇处理亚硒酸盐,制备丙酮酸乙酯取代苯腙; 使丙酮酸对取代苯腙与多磷酸在甲苯中反应制备5-取代的吲哚-2-羧酸酯; 并使5-取代的吲哚-2-羧酸乙酯与硫酸和乙酸或溴化氢的混合物反应,其中R是甲基,溴,氰基,羧基和甲氧基。