- Preparation method for morpholine-3-carboxylic acid
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The invention provides a preparation method for morpholine-3-carboxylic acid. The preparation method comprises the following steps: taking (2-Hydroxyethyl)carbamic acid tert-butyl ester and 2-chloroacrylonitrile as raw materials, performing Michael addition reaction, performing deprotection reaction, performing ring-closure reaction, and performing hydrolysis reaction to obtain the morpholine-3-carboxylic acid. The preparation method for the morpholine-3-carboxylic acid provided by the invention is used for preparing morpholine-3-carboxylic acid through Michael addition reaction, the deprotection reaction, ring-closure reaction and hydrolysis reaction; the whole preparation process is simple, is fewer in steps, adopts cheap and easily available raw materials, is free of stimulus and easilyallergic substances, and avoids generating highly toxic products and side products; and the yield of reaction at each step can be 80% or higher, the total yield is high, large-scale production is facilitated, economic benefits are improved, and the market value is good.
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- Preparation method N-t-butyloxycarboryl morpholine-3-carboxylic acid
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The invention provides a preparation method of N-t-butyloxycarboryl morpholine-3-carboxylic acid. According to the preparation method, 1,2-epoxypropane is taken as a raw material, ring-opening reaction, cyclization reaction, hydrolysis reaction, and nitrogen protection reaction are carried out successively so as to obtain N-t-butyloxycarboryl morpholine-3-carboxylic acid, wherein the ring-openingreaction is carried out under catalytic effect of transition metal Lewis acid. Reaction conditions are mild; operation is simple; no severely toxic side product is generated; the reaction yield of each step is 80% or higher; the reaction yield of a part reaction steps is 90% or higher; the yield is high; the preparation method is beneficial for large scale production, and is high in market value.
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Paragraph 0052; 0061-0063; 0069; 0078-0080; 0086; 0095-0097
(2018/07/30)
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- Synthesis of 3-oxadiazolyl/triazolyl morpholines: Novel scaffolds for drug discovery
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Synthesis of isomeric 3-oxadiazolyl/triazolyl morpholines was performed based on a common intermediate on the gram scale. The target compounds were designed as novel scaffolds for the medicinal chemistry. The key reaction was an electrochemical CH-oxidati
- Tereshchenko, Alexander D.,Myronchuk, Julia S.,Leitchenko, Lena D.,Knysh, Irina V.,Tokmakova, Ganna O.,Litsis, Olena O.,Tolmachev, Andrey,Liubchak, Konstantin,Mykhailiuk, Pavel
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p. 750 - 757
(2017/01/16)
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- N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
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N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
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- N2 -arylsulfonyl-l-argininamides and the pharmaceutically acceptable salts thereof
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N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
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- N2 -arylsulfonyl-argininamides and the pharmaceutically acceptable salts thereof
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N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
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- N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
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N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
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