775-16-6Relevant articles and documents
Synthesis method of 3-aminopyrrolidine dihydrochloride
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, (2022/04/20)
The invention discloses a synthetic method of 3-aminopyrrolidine dihydrochloride. The synthetic method comprises the following steps: preparing benzyl-(3-ethoxy-3-alkenyl)-(1-vinyl ethoxy methyl) amine liquid; preparation of a 1-benzyl-3-pyrrolidone solution; preparation of a 1-benzyl-3-aminopyrrolidine solution; preparing a 1-benzyl-3-aminopyrrolidine salt; preparing a 3-aminopyrrolidine solution; the yield and purity of the 3-aminopyrrolidine dihydrochloride are improved by controlling the activity of the reaction main materials of each part in a segmented manner and carrying out a directional hydrogenation manner.
Preparation method of 5-benzyl-5-N spiro[2. 4]heptane-1-carboxylic acid
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Paragraph 0026-0031, (2017/08/31)
The invention discloses a preparation method of 5-benzyl-5-N spiro[2. 4]heptane-1-carboxylic acid. The preparation method comprises that through a series of Swern oxidation reaction, Wittig reaction, sulfur ylide reaction and hydrolysis reaction, 5-benzyl-5-N spiro[2. 4]heptane-1-carboxylic acid is prepared from 1-benzyl-3-hydroxypyrrolidine. The preparation method utilizes a reaction of the double bond and the sulfur ylide to produce the ternary ring, utilizes cheap and easily available raw materials, has mild conditions, utilizes a simple operation way and greatly improves the possibility of industrialization.
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors
Bekkali, Younes,Thomson, David S.,Betageri, Raj,Emmanuel, Michel J.,Hao, Ming-Hong,Hickey, Eugene,Liu, Weimin,Patel, Usha,Ward, Yancey D.,Young, Erick R.R.,Nelson, Richard,Kukulka, Alison,Brown, Maryanne L.,Crane, Kathy,White, Della,Freeman, Dorothy M.,Labadia, Mark E.,Wildeson, Jessi,Spero, Denice M.
, p. 2465 - 2469 (2008/03/11)
The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.