CAS: 5987-82-6; Oxybuprocaine Hydrochloride

上下游产品

ethyl 3-hydroxy-4-nitro-benzoate benoxinate methyl 3-hydroxy-4-nitrobenzoate methyl 3-butoxy-4-nitrobenzoate

Ethyl 3-Butoxy-4-Nitrobenzoate置于iron(Iii) Chloride,Potassium Carbonate,甲烷,一水合肼,Sodium Hydroxide体系中,用 乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 13.0H,反应生成 奥布卡因盐酸盐
参考文献:一种盐酸奥布卡因的制备方法
标题:一种盐酸奥布卡因的制备方法
摘要:本发明公开了一种盐酸奥布卡因的制备方法.所述制备方法包括如下步骤:在碱ⅰ存在的条件下,3‑羟基‑4‑硝基苯甲酸乙酯与溴丁烷经亲电取代反应得到3‑丁氧基‑4‑硝基苯甲酸乙酯;在碱性条件下,3‑丁氧基‑4‑硝基苯甲酸乙酯进行水解反应,调节所述水解反应后的体系的ph值至1~3,得到3‑丁氧基‑4‑硝基苯甲酸;在碱ⅱ存在的条件下,3‑丁氧基‑4‑硝基苯甲酸与二乙氨基氯乙烷经亲电取代反应得到4‑硝基‑2‑丁氧基苯甲酸‑2‑(二乙氨基)乙酯,再在三氯化铁和水合肼的作用下经还原反应即得.本发明方法采用3‑羟基‑4‑硝基苯甲酸乙酯作为原料,经过4步常规的反应即得到目标产物;每步反应不需要在高压的条件下进行,且所需原料均为常规的化合物,易得且成本较低.

专利信息

专利号:US-7067554-B2
优先权日:2000-05-30
标 题 :Method for the synthesis of compounds of formula I and their uses thereof
发明人：MJALLI ADNAN M M; GOPALASWAMY RAMESH; AVOR KWASI A; WYSONG CHRISTOPHER L; ANDREW PATRON
权利人:TRANSTECH PHARMA INC
摘要:This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

专利号:US-2007203079-A1
优先权日:2005-11-21
标题:Methods of using small molecule compounds for neuroprotection
发明人：CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG
权利人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG
摘要:Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.

专利号:US-8076332-B2
优先权日:2006-12-26
标 题:N- (2-aminophenyl) benzamide derivative having urea structure
发明人：MOGI HIROYUKI; TAJIMA HISASHI; MISHINA NORIKO; YAMAZAKI YUSUKE; YONEDA SHINJI; WATANABE KATSUHIKO; FUJIKAWA JUNKO; YAMAMOTO MINORU
权利人:MOGI HIROYUKI; TAJIMA HISASHI; MISHINA NORIKO; YAMAZAKI YUSUKE; YONEDA SHINJI; WATANABE KATSUHIKO; FUJIKAWA JUNKO; YAMAMOTO MINORU; SANTEN PHARMACEUTICAL CO LTD
摘要:The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R 1 and R 2 represent a hydrogen atom, a lower alkyl group, or the like; R 3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R 4 and R 5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.

专利号:US-8012972-B2
优先权日:2007-03-28
标 题:Pyridinecarboxylic acid (2-aminophenyl) amide derivative having urea structure
发明人：MOGI HIROYUKI; TAJIMA HISASHI; MISHINA NORIKO; YAMAZAKI YUSUKE; YONEDA SHINJI; WATANABE KATSUHIKO; FUJIKAWA JUNKO; YAMAMOTO MINORU
权利人:SANTEN PHARMACEUTICAL CO LTD
摘要:Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, R 1 and R 2 represent a hydrogen atom, a lower alkyl group or the like; R 3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, a carboxy group, a lower alkoxycarbonyl group, —OCONR a R b , —NR c R d or the like; R 4 and R 5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; R a and R b represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group or the like; R c and R d represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group or the like; X represents a lower alkylene group; Y represents a single bond, a lower alkylene group; W 1 -W 2 represents N—C or C—N; and l and m represent 0, 1, 2 or 3.

专利号:US-2006189578-A1
优先权日:2000-05-30
标题:Method for the synthesis of compounds of formula I and their uses thereof

专利号:US-2004097407-A1
优先权日:2000-05-30
标题:Method for the synthesis of compounds of formula I and their uses thereof