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    • 7. 发明授权
    • 5-(치환된 페닐알킬)아미노살리실산 화합물의 제조 방법
    • 5-(치환된페닐알킬)아미노살리실산화합물의제조방5-
    • KR100639551B1
    • 2006-10-30
    • KR1020050068879
    • 2005-07-28
    • (주)에스에이치제약김수동
    • 양주환송용봉박경배박정호정승필이해언
    • C07C227/16
    • Provided is a method for preparing a 5-(substituted phenylalkyl)aminosalicylic acid compound from an alkyl 5-(substituted phenylalkyl)aminosalicylate as an intermediate to improve yield by preventing the generation of monomers and to lower cost. The method comprises the step of reacting an alkyl 5-(substituted phenylalkyl)aminosalicylate represented by the formula II with HCl to prepare a 5-(substituted phenyalkyl)aminosalicylic acid compound represented by the formula I by hydrolysis, wherein R is H, a halogen atom, a haloalkyl group, a nitro group, a hydroxy group, an alkyl group, an aryl group, an alkoxy group or an amine group; n is 1 or 2; A is H or an alkyl group; and B is H or an acetyl group. The alkyl 5-(substituted phenylalkyl)aminosalicylate of the formula II is prepared by reacting an R-substituted 2-phenyl acetaldehyde or 3-phenylpropyl aldehyde with 5-aminosalicylic acid by reductive amination.
    • 本发明提供一种从作为中间体的5-(取代苯基烷基)氨基水杨酸烷基酯制备5-(取代苯基烷基)氨基水杨酸化合物以通过防止产生单体来提高产率并降低成本的方法。 该方法包括使由式II表示的5-(取代的苯基烷基)氨基水杨酸烷基酯与HCl反应以通过水解制备式I表示的5-(取代的苯基烷基)氨基水杨酸化合物的步骤,其中R为H,卤素 原子,卤代烷基,硝基,羟基,烷基,芳基,烷氧基或胺基; n是1或2; A是H或烷基; B是H或乙酰基。 式II的5-(取代的苯基烷基)氨基水杨酸烷基酯是通过将R-取代的2-苯基乙醛或3-苯基丙醛与5-氨基水杨酸通过还原胺化反应制备的。
    • 10. 发明授权
    • 페닐아세톡시아세트산유도체의제조방법
    • KR100335852B1
    • 2003-02-11
    • KR1019980033954
    • 1998-08-21
    • 민연식
    • 민연식
    • C07C227/16
    • PURPOSE: Preparing method of the title compound is provided which has a shorten reaction time and high yield. CONSTITUTION: Sodium 2-£(2,6-dichlorophenyl)amino|phenylacetate and alkyl haloacetate (CH2XCOOR1; R1 is C1- C7 alkyl group) are reacted at -30- 80 degree C in lower aliphatic alcohol derivatives such as C1- C7 alcohol or its ester in the presence of alkali metal carbonate such as potassium carbonate, sodium carbonate and phase transfer catalyst such as benzyl triethyl ammonium chloride, tetrabutyl ammonium bromide, tetrabutyl ammonium hydrogen sulfate, methyl trioctyl ammonium bromide, etc. and 18-crown-6. Obtained product is hydrolyzed at -30- 80 degree C for 2-8 hours in solvent such as C1-C4 alcohol, formic acid, acetic acid, propionic acid, butyric acid in the presence of catalyst such as inorganic conc. sulfuric acid or p-toluene sulfonic acid to give the title compound(I; R is hydrogen or C1- C7 alkyl group).
    • 用途:提供了缩短反应时间和提高收率的标题化合物的制备方法。 构成:2-(2,6-二氯苯基)氨基乙酸苯酯和卤代乙酸烷基酯(CH 2 XCOOR 1; R 1是C 1 -C 7烷基)在-30-80℃在低级脂族醇衍生物例如C 1 -C 7 醇或其酯在碱金属碳酸盐如碳酸钾,碳酸钠和相转移催化剂如苄基三乙基氯化铵,四丁基溴化铵,四丁基硫酸氢铵,甲基三辛基溴化铵等存在下进行反应和18-冠醚 - 6。 得到的产物在溶剂如C1-C4醇,甲酸,乙酸,丙酸,丁酸中,在催化剂如无机浓缩物存在下于-30-80℃水解2-8小时。 硫酸或对甲苯磺酸反应,得到标题化合物(I; R是氢或C 1 -C 7烷基)。