- Preparation method of 4-morpholinyl-2-ethylpiperazine
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The invention discloses a preparation method of 4-morpholinyl-2-ethylpiperazine. The method comprises the following steps: (1) putting 2-hydroxyethylpiperazine and thionyl chloride into a first solvent, and performing a reaction to convert hydroxyl groups into chlorine to obtain a first reaction product; (2) putting the first reaction product obtained in step (1) and boc anhydride into a second solvent, and performing a reaction to obtain an N-boc protected second reaction product; (3) putting the second reaction product obtained in step (2), morpholine and an acid-binding agent into a third solvent at 20-50 DEG C, and performing a reaction to obtain a third reaction product; and (4) dissolving the third reaction product obtained in step (3) and an alkali in a fourth solvent, heating the obtained solution to 40-80 DEG C, performing a reaction for about 10-20 h, concentrating the obtained reaction solution, and extracting and concentrating the obtained concentrate to obtain the 4-morpholinyl-2-ethylpiperazine. Raw materials used in the method are cheap and are easy to obtain, the operation process is simple, and the purity of the obtained product is high and exceeds 99%.
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- Substituted formyldimethomorph (ethylpiperazine compound and) application thereof
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The invention relates to substituted formyl morpholinoethyl piperazine compounds and an application thereof. The compounds are shown in a general formula (I) in the description, wherein R is phenyl, pyridyl, furyl, pyrazolyl, thiazolyl, thienyl or phenazi
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Paragraph 0040-0043
(2020/01/31)
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- CARBODITHIOATES WITH SPERMICIDAL ACTIVITY AND PROCESS FOR PREPARATION THEREOF
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The present invention relates to the synthesis and biological evaluation of compound of formula I as spermicidal agents, and its pharmaceutically acceptable acid salt thereof. The invention provides bis(4- substituted-1-piperazinylthiocarbonyl) disulfide (when n = 0) and alkane-1,n-diylbis(4-substituted piperazine-1-carbodithioate) (when n = 0, 1, 2 or 3) as shown in figure 1 of the accompanying drawing. These compounds are found to be useful for spermicidal activity.
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Page/Page column 30
(2014/08/20)
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- Natural product-based design, synthesis and biological evaluation of anthra[2,1-d]thiazole-6,11-dione derivatives from rhein as novel antitumour agents
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Two series of novel 2-substituted 5,7-dihydroxyanthra[2,1-d]thiazole-6,11- dione derivatives from natural rhein were designed, synthesized and evaluated for their antitumour activities against human cancer cell lines A549 and HeLa in vitro.
- Liang, Yu-Kun,Yue, Zhi-Zhou,Li, Jia-Xin,Tan, Cun,Miao, Ze-Hong,Tan, Wen-Fu,Yang, Chun-Hao
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p. 505 - 515
(2014/08/05)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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