- Preparation method for 2-(2-methoxyphenoxy)ethylamine
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The invention provides a preparation method for 2-(2-methoxyphenoxy)ethylamine. The preparation method comprises the following steps: synthesizing 2-(2-methoxyphenoxy)ethanol with guaiacol as a starting material; then synthesizing 2-(2-methoxyphenoxy)chloroethane through chlorination; then reacting 2-(2-methoxyphenoxy)chloroethane with potassium phthalimide to obtain N-(o-methoxyphenoxyethyl)-phthalimide; and finally, performing basic hydrolysis to obtain 2-(2-methoxyphenoxy)ethylamine. The yields of the above four steps of reactions are that the yield of 2-(2-methoxyphenoxy)ethanol is 98.9%;the yield of 2-(2-methoxyphenoxy)chloroethane is 93.7%; the yield of N-(o-methoxyphenoxyethyl)-phthalimide is 86.4%; the yield of 2-(2-methoxyphenoxy)ethylamine is 91.2%; and the total yield of the four steps is 73.04%, which is higher than the yield of 43% in conventional production processes. The preparation method of the invention reduces the production cost of 2-(2-methoxyphenoxy)ethylamine and is safe in the production process.
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Paragraph 0015
(2019/01/24)
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- Formononetin derivatives and preparation methods and medical application thereof
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The invention relates to the field of pharmaceutical chemistry, and relates to formononetin derivatives and preparation methods and medical application thereof, in particular to formononetin derivatives with the general formula as shown in (I), preparation methods thereof, pharmaceutical compositions containing the compounds and medical application of the derivatives and the pharmaceutical compositions, particularly, application of the derivatives and the pharmaceutical compositions serving as drugs for preventing or treating hyperlipidaemia or obesity or type-II diabetes. Please see the formula in the description.
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Paragraph 0132; 0133; 0134
(2017/04/29)
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- Pyrrolo[2,1-c][1,4]naphthodiazepine Linked Piperazine Compounds and a Process for the Preparation Thereof
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The present invention provides a compound of general formula A, useful as potential antitumour agents against five human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]naphthodiazepine linked substituted piperazine conjugates attached through different alkane spacers of general formula A. (Formula I) General formula A. Where R=R′=(Formula II). n=1-9 and R″=methyl, ethyl, acetyl, benzyl, piperinoyl, 4-fluorophenyl, 4-chlorophenyl, 4-methoxyphenyl, pyridyl, pyrimidyl
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Paragraph 0273
(2013/12/04)
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- Synthesis of racemic and chiral Carvedilol starting from corresponding 5-(chloromethyl)oxazolidin-2-one
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The synthesis of racemic Carvedilol ((±)-1) has been achieved starting from 2-(chloromethyl) oxirane ((±)-2) in a four-step sequence. 5-(Chloromethyl) oxazolidin-2-one ((±)-3) and 5-((9Hcarbazol-4-yloxy) methyl) oxazolidin-2-one ((±)-4) are intermediates. A similar sequence starting from (R)- or (S)-2-(chloromethyl)oxirane 2 give corresponding chiral 5-((9Hcarbazol-4-yloxy)methyl) oxazolidin-2-one 4 followed by chiral Carvedilol 1. The synthetic sequence followed avoids the formation of impurity B (bis impurity). This approach can be useful for the preparation of pharmaceutically important moieties containingβ-amino alcohols without formation of bis impurity.
- Anand Kumar,Veera Babu,Rao, Rama Koteshwar,Srinivas, Kumbam,Madhusudhan,Mukkanti
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p. 1430 - 1435
(2012/11/06)
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- A facile synthesis of carvedilol via β-amino alcohol intermediate
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A facile synthesis of Carvedilol via a key β-amino alcohol intermediate is described and this approach avoids the formation of bis side product (impurity B).
- Tatendra Reddy,Suneel Kumar,Omprakash,Dubey
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p. 251 - 254
(2013/09/24)
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- PYRROLO [2,1-C]1,4]NAPHTHODIAZEPINE LINKED PIPERAZINE COMPOUNDS AND A PROCESS FOR THE PREPARATION THEREOF
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The present invention provides a compound of general formula A, useful as potential antitumour agents against five human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]naphthodiazepine linked substituted piperazine conjugates attached through different alkane spacers of general formula A. (Formula I) General formula A. Where R= R'= (Formula II). n=1-9 and R''= methyl, ethyl, acetyl, benzyl, piperinoyl, 4-fluorophenyl, 4-chlorophenyl, 4-methoxyphenyl, pyridyl, pyrimidyl
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Page/Page column 42
(2012/09/10)
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- Synthesis of impurity A in Carvedilol: a β-adrenergic receptor
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Carvedilol is prepared by different synthetic approaches. Almost in all the approaches the major impurities that are known in the literature A, B, C, D and E are listed in European pharmacopoeia. The control of pharmaceutical impurities is currently a critical issue to the pharmaceutical industry. In this publication, a description of these impurities and their origins in Carvedilol process are presented along with the preparation of impurity A.
- Madhusudhan,Naidu,Kumar,Satyanarayana,Balraju
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experimental part
p. 741 - 745
(2009/12/24)
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- PREPARATION OF 2-(2-ALKOXY PHENOXY) ETHYLAMINE, AN INTERMEDIATE OF CARVEDILOL AND TAMSULOSIN
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The present patent application relates to a process for the preparation of 2-(2-Alkoxy phenoxy) ethylamine or a salt thereof, which is a useful intermediate in the preparation of several active pharmaceutical ingredients including Carvedilol and Tamsulosin. It also provides 2-(2-methoxy phenoxy) ethylamine in solid form.
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Page/Page column 9; 10
(2009/12/02)
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- APORPHINE AND OXOAPORPHINE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
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The invention provides aporphine and oxoaporphine compounds that may be used to manufacture a medicaments for preventing or treating vascular dysfunction resulting in ischemic and metabolic diseases or preventing complications in human and mammal. The isc
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Page/Page column 27; 30
(2008/06/13)
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- 4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors
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It has been previously reported that appropriately substituted 4-anilinoquinoline-3-carbonitriles are potent inhibitors of Src kinase, with biological activity in vitro and in vivo. Structural modifications to these compounds have been explored, providing
- Berger, Dan M.,Dutia, Minu,Birnberg, Gary,Powell, Dennis,Boschelli, Diane H.,Wang, Yanong D.,Ravi, Malini,Yaczko, Deanna,Golas, Jennifer,Lucas, Judy,Boschelli, Frank
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p. 5909 - 5920
(2007/10/03)
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- Tricyclic protein kinase inhibitors
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This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyro sine kinase and are antiproliferative agents.
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