134136-04-2Relevant academic research and scientific papers
Pd-Catalyzed Highly Chemo- And Regioselective Hydrocarboxylation of Terminal Alkyl Olefins with Formic Acid
Ren, Wenlong,Chu, Jianxiao,Sun, Fei,Shi, Yian
supporting information, p. 5967 - 5970 (2019/08/26)
An efficient Pd-catalyzed hydrocarboxylation of alkenes with HCOOH is described. A wide variety of linear carboxylic acids bearing various functional groups can be obtained with excellent chemo- and regioselectivities under mild reaction conditions. The reaction process is operationally simple and requires no handling of toxic CO.
Synthetic method of terminal carboxylic acid
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Paragraph 0119-0122, (2019/11/21)
The invention discloses a synthetic method of a terminal carboxylic acid. The synthetic method is characterized by comprising the steps of adding an olefin represented by a formula (3) shown in the description, formic acid, acetic anhydride, Pd(OAc)2 and a monophosphorus ligand TFPP into an organic solvent in a proportion, carrying out hydrogen carbonylation reaction on the olefin represented by the formula (3) shown in the description, formic acid and acetic anhydride at 80-90 DEG C for 48h-72h under the catalysis of the metal palladium salt Pd(OAc)2 and the monophosphorus ligand TFPP so as to obtain the terminal carboxylic acid represented by a formula shown in the description, and separating a target product, namely the terminal carboxylic acid after the reaction is finished, wherein olefin represented by the formula (3) is selected from cycloolefins, or linear olefins of which the R1 is electron donating groups. By virtue of the method disclosed by the invention, corresponding terminal carboxylic acid and a derivative thereof can be prepared through the reaction under mild conditions of low temperature and no high pressure; and the steps of the synthetic method are simple and convenient, the operation is convenient, the yield is high, the energy source can be greatly saved, and the synthetic efficiency can be greatly improved.
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl] cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors
Chen, Ping,Caldwell, Charles G.,Ashton, Wallace,Wu, Joseph K.,He, Huaibing,Lyons, Kathryn A.,Thornberry, Nancy A.,Weber, Ann E.
scheme or table, p. 1880 - 1886 (2011/05/05)
A series of 4-amino cyclohexanes and 4-substituted piperidines were prepared and evaluated for inhibition of DPP-4. Analog 20q displayed both good DPP-4 potency and selectivity against other proteases, while derivative 20k displayed long half life and mod
Inhibitors of Serine Proteases
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, (2010/12/26)
The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.
INHIBITORS OF SERINE PROTEASES FOR THE TREATMENT OF HCV INFECTIONS
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Page/Page column 472, (2008/12/07)
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.
NEW CARBONYLATED (AZA)CYCLOHEXANES AS DOPAMINE D3 RECEPTOR LIGANDS
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Page/Page column 94, (2008/06/13)
The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
Antibiotic-Bound Poly(Caprolactone) Polymer
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Page/Page column 3, (2008/06/13)
This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After polymerization, the protecting group can be removed and an antibiotic can be attached as a new pendant group. The bioactivity of the antibiotic-bound poly(caprolactone) polymer is described.
INHIBITORS OF SERINE PROTEASES
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Page/Page column 303, (2010/11/26)
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.
N-SUBSTITUTED PHENYLACETAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 107, (2008/06/13)
A compound represented by the formula: (I) wherein R1 represents a methoxy group, a hydroxyl group or a hydrogen atom; R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylcarbonyl group or an arylcarbonyl group; and D represents a group represented by the formula (A), (B) or (C) below. (A) (B) (C) This compound is useful as a therapeutic agent for a pain or inflammation induced by any one of various morbid conditions such as neuropathic pain, rheumatoid arthritis and osteoarthritis.
NEW DERIVATIVES OF PYRIDIL PIPERAZINE OR PYRIDAZINYL PIPERAZYL, PROCESS FOR PRODUCTION THEREOF AND MEDICAMENTS CONTAINING THESE COMPOUNDS
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, (2008/06/13)
Compounds of formula I in which R1 denotes hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, an optionally substituted monocyclic or bicyclic aryl, an optionally substituted hetaryl, an optionally substituted arylalkyl or one of the groups —OR2, —NR3R4, W denotes nitrogen or X, Z independently of one another denote nitrogen or CH and in the case that W denotes a nitrogen atom, X must be the group, A denotes a valency dash or a carbonyl group, B denotes a valency dash or a C1-C6 alkylene chain optionally substituted once or several times by lower alkyl or an OR2 group, D denotes a valency dash and, in the case that X is a nitrogen atom, can also be a carbonyl group in which case A, B and D may not simultaneously denote a valency dash, R2 denotes hydrogen, lower alkyl or arylalkyl, R3 and R4 independently of one another denote hydrogen or lower alkyl or together with the nitrogen atom to which they are bound form a five to six-membered heterocyclic ring, R5 denotes hydrogen or a group OR2, processes for the production thereof as well as pharmaceutical agents containing these compounds for the treatment of diseases which are the result of thrombo-embolic events.
