- Preparation method of 1-amino-1-cyclopropanecarbonitrile hydrochloride
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The invention discloses a preparation method of 1-amino-1-cyclopropanecarbonitrile hydrochloride and belongs to the technical field of organic synthesis. In the method, nitroacetonitrile is used as aninitial raw material and is reacted with 1,2-dihalogenated ethane under catalysis of an alkali to produce 1-nitro-1-cyclopropanecarbonitrile, which is then subjected to a nitro-reduction reaction toprepare the 1-amino-1-cyclopropanecarbonitrile hydrochloride. The method has gentle conditions and high yield, is low in cost and is suitable for industrial application.
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Paragraph 0010; 0012; 0014; 0016; 0018; 0020; 0022; 0024
(2018/03/26)
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- A 1 - amino - 1 - propionitrile hydrochloride synthetic method (by machine translation)
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The invention discloses a 1 - amino - 1 - propionitrile hydrochloride synthetic method, the method utilizes the amino acetonitrile as a starting material with benzene sulfonyl chloride reaction to obtain N, N - phenyl sulfonyl acetonitrile, continue to sodium hydride under alkaline conditions with 1, 2 - Dibromoethane ring reaction to obtain N, N - phenyl sulfonyl amino link propyl nitrile, finally removing benzoyl protection under the acidic condition to obtain the 1 - amino - 1 - propionitrile hydrochloride. The invention mild reaction conditions, high yield, low cost and is suitable for industrial application. (by machine translation)
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Paragraph 0012; 0015
(2018/03/26)
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- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 52
(2010/06/15)
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- DI-FLUORO CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 38-39
(2009/10/30)
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- DI-FLUORO CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 34-35
(2008/06/13)
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- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 49-50
(2008/06/13)
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- SULFONAMIDE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds of formula ( I ) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is-alkylene-SO2NR5R6.
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Page/Page column 73
(2008/06/13)
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- PROCESSES AND INTERMEDIATES FOR PREPARING CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to a novel process for preparing certain cysteine protease inhibitors.
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Page/Page column 63
(2010/10/20)
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- SULFONYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 59
(2010/11/24)
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- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 62
(2008/06/13)
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- SILINANE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them. The present invention is also directed to the use of these inhibitors in combination with a therapy that causes a deleterious immune response in patients receiving the therapy.
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Page/Page column 63-64
(2008/06/13)
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- Latent Inhibitors. Part 8. Synthesis and Evaluation of some Mechanism-based Inhibitors of Dihydrofolate Reductase
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The synthesis of two new pteridine-7-spirocyclopropanes that are time-dependent irreversible inhibitors of dihydrofolate reductase is described.Several related compounds including a cyclopropyl substituted quinoxaline and 2-aminopteridine-4(3H),6(5H)-dione were also prepared but these compounds were not found to be time-dependent inhibitors.The inhibitors were assessed using several dihydrofolate reductases, Escherichia coli RT/39, two mutants of the E. coli enzyme, Lactobacillus casei, and chicken liver.Activity was found against all enzymes tested but most strongly against E. coli wild type enzyme.
- McGill, John,Rees, Lilias,Suckling, Colin J.,Wood, Hamish C. S.
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p. 1299 - 1304
(2007/10/02)
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- A New and Convenient Preparation of 1-Aminocyclopropanecarboxylic Acid from Acrolein
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Cyclopropanecarboxylic acid 3 and cyclopropanone hemiacetal 4 have been tested as possible convenient precursors of the α-aminocyclopropanecarboxylic acid (1), an immediate biosynthetic source of ethylene, the phytohormone which regulates plant growth.While acid 3 was aminated only in low yield and hemiacetal 4 did not submit to the Strecker synthesis, the benzophenone imine of 2-amino-4-chlorobutyronitrile 5, readily available from acrolein, did undergo quantitative base-induced cyclization smoothly under various conditions.
- Salauen, Jacques,Marguerite, Jacqueline,Karkour, Belkacem
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p. 4276 - 4281
(2007/10/02)
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