CAS: 99-43-4; 2-(Diethylamino)Ethyl 4-Amino-3-Butoxybenzoate

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CAS号72101-53-2 3-丁氧基-4-硝基苯甲酸 | CAS号100-37-8 二乙氨基乙醇 | CAS号23442-22-0 4-氨基-3-丁氧基苯甲酸

📜3-羟基-4-硝基苯甲酸甲酯置于水,铁粉,Potassium Carbonate,Sodium Hydroxide体系中,用 正庚烷,丁酮 作为反应溶剂,化学反应 15.0H,反应生成 丁氧卡因
参考文献:一种盐酸奥布卡因的合成方法
标题:一种盐酸奥布卡因的合成方法
摘要:本发明公开了一种盐酸奥布卡因的合成方法,包括如下步骤:(1)式ⅱ所示化合物与1‑溴丁烷进行醚化反应,制得式ⅲ所示化合物;(2)式ⅲ所示化合物与2‑(二乙氨基)乙醇在催化剂作用下进行酯交换反应,成盐,制得式ⅳ所示化合物;(3)式ⅳ所示化合物与还原剂进行还原反应,得到式ⅴ所示奥布卡因游离碱;(4)式ⅴ所示奥布卡因游离碱经成盐反应,析晶,得到式ⅰ所示盐酸奥布卡因.本发明所提的盐酸奥布卡因的合成方法,合成路线步骤长度合适,三步反应一步成盐,且没有高温高压反应,对于设备的要求不高,适合工业化生产.

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:AU-2005200425-A1
优先权日:2000-05-30
标题 :A method for the synthesis of compounds of formula 1 and their uses thereof

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-8927485-B2
优先权日:2010-02-18
标题:Site-specific modification of proteins through chemical modification enabling protein conjugates, protein dimer formation, and stapled peptides
发明人：KRANTZ ALEXANDER; YU PENG
权利人:KRANTZ ALEXANDER; YU PENG; ADVANCED PROTEOME THERAPEUTICS INC
摘要:The present invention generally provides methods for the site-specific modification of peptides, polypeptides, and proteins, e.g., granulocyte macrophage colony-stimulating factor, human superoxide dismutase, annexin, leptin, antibodies and the like, cytokines and chemokines, at their N-termini and at sites at which unnatural aminoacids have been introduced along the protein framework. The modifications described herein can be used for the synthesis and application of the adducts in radio-labeling, molecular imaging and protein therapeutic applications, and the treatment of disorders such as rheumatoid arthritis, lupus erythematosus, psoriasis, multiple sclerosis, type-1 diabetes, Crohn's disease, and systemic sclerosis, Alzheimer disease, cancer, liver disease (e.g., alcoholic liver disease), and cachexia.