- Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease
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Multitarget molecular hybrids of N-benzyl pyrrolidine derivatives were designed, synthesized, and biologically evaluated for the treatment of Alzheimer's disease (AD). Among the synthesized compounds, 4k and 4o showed balanced enzyme inhibitions against c
- Choubey, Priyanka Kumari,Sharma, Piyoosh,Shrivastava, Sushant Kumar,Tripathi, Avanish
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- 3-aminopyrrolidine hydrochloride synthesis method
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The invention relates to the technical field of organic synthesis, in particular to a 3-aminopyrrolidine hydrochloride synthesis method which includes the steps: performing amination reaction on maleic anhydride and R1NH2, and performing dehydration to obtain N-substituted maleimide as shown in a formula (I); performing addition reaction on the N-substituted maleimide and R2NH2 to obtain N-substituted pyrrolidine-2, 5-diketone as shown in a formula (II); reducing the N-substituted pyrrolidine-2, 5-diketone by reducing agents under nitrogen protection to obtain N-substituted pyrrolidine-3-amineas shown in a formula (III); performing hydrogenation reaction on the N-substituted pyrrolidine-3-amine under the action of catalysts to obtain 3-aminopyrrolidine as shown in a formula (IV); salifying the 3-aminopyrrolidine and hydrochloric acid to obtain 3-aminopyrrolidine hydrochloride as shown in a formula (V). R1 and R2 are independently alkyl, aryl, aralkyl, alkyl sulfonyl, aryl sulfonyl oralkoxycarbonyl. The synthesis method is simple in process, low in cost, high in yield and less in pollution.
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Paragraph 0054; 0062; 0069-0071; 0072-0074
(2019/03/08)
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- CHEMICAL COMPOUNDS
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The present invention provides compounds of formula (I) wherein R1 to R6 and m are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Mo
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Page/Page column 35-36
(2008/06/13)
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- 3-Aminopyrrolidine lithium amide in enantioselective: Addition of organolithium compounds onto aromatic aldehydes
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New N,N'-disubstituted-3-aminopyrrolidines lithium amides have been used as chiral auxiliaries in the asymmetric condensation of n-butyllithium onto aromatic aldehydes, leading to e.e.s up to 73%.
- Corruble, Aline,Valnot, Jean-Yves,Maddaluno, Jacques,Duhamel, Pierre
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p. 1519 - 1523
(2007/10/03)
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- Handy access to chiral N,N'-disubstituted 3-aminopyrrolidines
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A new and rapid synthesis of (S)-3-aminopyrrolidines Z is proposed from N-protected (S)-Asparagine. Basic cyclization of methyl N-Z-(S)-Asparaginate 1 followed by one-pot N-benzylation directly leads to (S)-aminosuccinimide 3 which, after cleavage of the
- Maddaluno,Corruble,Leroux,Ple,Duhamel
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p. 1239 - 1242
(2007/10/02)
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- Process for preparing 3-amino-1-benzylpyrrolidines
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A process for preparing a 3-amino-1-benzyl-pyrrolidine of the formula STR1 in which R1 and R2 each independently is H or alkyl, and Ph is phenyl, comprising reacting a 1-benzyl-Δ3 -pyrroline-2,5-dione of the formula STR2 in which R3 and R4 each independently is H or alkyl, with a nitrogen nucleophile of the formula in which R5 is H, benzyl, naphthylmethyl or phenyl-CHR6, and R6 is C1 -C6 -alkyl or phenyl, to give an optionally substituted 3-amino-1-benzylpyrrolidine-2,5-dione of the formula STR3 and, if R5 ≠H, the protecting group R5 is subsequently cleaved off to give a 3-amino-1-benzylpyrrolidine-2,5-dione of the formula STR4 and completely reducing the carbonyl groups to form the 3-amino-1-benzylpyrrolidine of the formula (I).
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- 3-aminopyrrolidine compound and process for preparation thereof
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Disclosed is a novel compound of 3-aminopyrrolidine having the formula (I): STR1 in which R1 is hydrogen, an alkyl, an aralkyl or an aryl.
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