CAS: 94-09-7; Ethyl 4-Aminobenzoate

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合成工艺路线路线简述

  • 合成目标产物 Benzocaine 主要起始原料 Ethyl 4-Azidobenzoate
  • (文献来源)合成步骤主要原料 Ethyl 4-Azidobenzoate
在 偶氮二异丁腈,三正丁基氢锡体系中,用 正己烷,甲苯,乙腈 作为反应溶剂,化学反应 21.0H,以87%的收率获得产物苯佐卡因
参考文献:2-(苯基硒基)乙烷磺酰胺作为苯胺的新型保护基,可通过自由基反应脱保护
标题:2-(苯基硒基)乙烷磺酰胺作为苯胺的新型保护基,可通过自由基反应脱保护
摘要:通过2-氯磺酰氯进行磺酰化,然后共轭加入苯硒酚,苯胺被保护为2-(苯基硒代)乙烷磺酰苯胺(sees苯胺).在aibn存在下,使用氢化三丁基锡通过自由基还原将sees苯胺脱保护.当将氢化物和aibn缓慢添加到系统中时,可以高收率获得相应的苯胺.由于自由基反应在中性条件下进行,因此实现了sees基团的化学选择性脱保护.sees苯胺在各种条件下(包括某些恶劣条件)都稳定.
DOI:10.1016/j.Tetlet.2016.05.002

海关参考信息

专利信息


专利号:WO-8400363-A1
优先权日:1982-07-12
标题 :Synthesis of periplanone-b
发明人:STILL W CLARK
权利人:HERCULITE PRODUCTS INC
摘要:A synthesis of periplanone-B, a female sex pheromone of the American cockroach, P. americana. Novel compounds which are useful as intermediates in the synthesis of periplanone-B are described including the precursor alcohol, periplanol-B.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-8058477-B2
优先权日:2006-03-21
标 题 :Process for the synthesis of arylamines from the reaction of an aromatic compound with ammonia or a metal amide
发明人:HARTWIG JOHN F; SHEN QILONG
权利人:HARTWIG JOHN F; SHEN QILONG; UNIV YALE
摘要:A catalytic process for the synthesis of aromatic primary amines, reagent compositions for effecting the process, and transition metal complexes useful in the process, are provided.

专利号:US-7598291-B2
优先权日:2004-09-02
标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin
发明人:NIMNI MARCEL; HAN BO
权利人:NIMNI MARCEL; HAN BO
摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.

专利号:US-2010160244-A1
优先权日:2004-09-02
标 题 :Methods and compositions for enhancing collagen, proteoglycan, and glutathione synthesis in the skin
发明人:NIMNI MARCEL; HAN BO
权利人:NIMNI MARCEL; HAN BO
摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids or hydrolyzed whey protein; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid or a lipoic acid analogue or derivative. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.

专利号:US-2003050305-A1
优先权日:2000-05-22
标题:Thromboxane inhibitors, compositions and methods of use
发明人:TEJADA INIGO SAENZ DE
摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, and, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.
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合成参考文献

合成方法参考DOI号:10.1002/chem.200903511
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