95798-22-4Relevant academic research and scientific papers
Carbamate Synthesis Using a Shelf-Stable and Renewable C1 Reactant
Dobi, Zoltán,Reddy, B. Narendraprasad,Renders, Evelien,Van Raemdonck, Laurent,Mensch, Carl,De Smet, Gilles,Chen, Chen,Bheeter, Charles,Sergeyev, Sergey,Herrebout, Wouter A.,Maes, Bert U. W.
, p. 3103 - 3114 (2019/06/24)
4-Propylcatechol carbonate is a shelf-stable, renewable C1 reactant. It is easily prepared from renewable 4-propylcatechol (derived from wood) and dimethyl carbonate (derived from CO2) using a reactive distillation system. In this work, the 4-propylcatechol carbonate is used for the two-step synthesis of carbamates under mild reaction conditions. In the first step, 4-propylcatechol carbonate is treated with an alcohol at 50–80 °C in the presence of a Lewis acid catalyst, such as Zn(OAc)2?2 H2O. With liquid alcohols, no solvent is used and with solid alcohols 2-methyltetrahydrofuran is used as solvent. In the second step, the alkyl 2-hydroxy-propylphenyl carbonate intermediates obtained react with amines at room temperature in 2-methyltetrahydrofuran, forming the target carbamates and the byproduct 4-propylcatechol, which can be recycled into a carbonate reactant.
Preparation method of 3-hydroxypiperidine, preparation method of derivative of 3-hydroxypiperidine, and intermediate of 3-hydroxypiperidine
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Paragraph 0073; 0074; 0075; 0076, (2017/08/27)
The invention discloses a preparation method of 3-hydroxypiperidine, a preparation method of a derivative of 3-hydroxypiperidine, and an intermediate of 3-hydroxypiperidine. The preparation method of 3-hydroxypiperidine (I) is characterized in that 5-halo-2-hydroxypentylamine halogen acid salt (III) undergoes a ring closure reaction in water under the action of an inorganic alkali to obtain the 3-hydroxypiperidine (I). The preparation method of N-protected 3-hydroxypiperidine (II) comprises the following steps: 1, 5-halo-2-hydroxypentylamine halogen acid salt (III) undergoes the ring closure reaction in water under the action of the inorganic alkali to obtain the 3-hydroxypiperidine (I); and 2, the 3-hydroxypiperidine (I) and a nitrogen protection reagent undergo an N-acylation reaction in an organic solvent under the action of the inorganic alkali to obtain the N-protected 3-hydroxypiperidine (II). The preparation methods have the advantages of simple operation, no expensive catalysts, low production cost, easily available raw materials, simplicity in operation, high reaction conversion rate, high selectivity, simple process, and suitableness for industrial production.
Stereo-complementary bioreduction of saturated N-heterocyclic ketones
Li, Chao,Liu, Yan,Pei, Xiao-Qiong,Wu, Zhong-Liu
, p. 90 - 97 (2017/04/28)
The asymmetric bioreduction of several saturated N-heterocyclic ketones is demonstrated in a stereo-complementary fashion using the ketoreductases READH and ChKRED20 for the production of (S)- and (R)-alcohols, respectively. The reaction accepts substrates with a five-, six- or seven-membered ring, and exhibits excellent stereoselectivity when using 2-propanol as both the ultimate reducing agent and cosolvent, achieve >99% ee in the majority of cases for both enantiomers.
PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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Page/Page column 44; 45, (2014/01/17)
The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
BRUTON'S TYROSINE KINASE INHIBITORS
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Page/Page column 75; 15, (2014/05/24)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
A library of conformationally restricted saturated heterocyclic sulfonyl chlorides
Zhersh, Sergey,Buryanov, Volodymyr V.,Karpenko, Oleksandr V.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
scheme or table, p. 3669 - 3674 (2011/12/16)
An approach to the synthesis of conformationally restricted saturated heterocyclic sulfonyl chlorides is described. Being guided by the principle of diversity-oriented conformational restriction, a mini-library of saturated heterocyclic sulfonyl chlorides
ARYLALKYLAMINES AND PROCESS FOR PRODUCTION THEREOF
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Page/Page column 35, (2010/11/25)
The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensiing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc. The symbols in the formula represent the following meanings: Ar: optionally substituted aryl or optionally substituted heteroaryl here, the cyclic portion of the heteroaryl is bicyclic heterocyclic ring in which 5- to 6-membered monocyclic heterocyclic ring containing 1 or 2 hetero atom(s) and benzene ring are fused; R 1 : a group selected from the group consisting of optionally substituted cyclic hydrocarbon group, and optionally substituted heterocyclic group; n: an integer of 1 to 3; X: single bonding arm, -CH 2 -, -CO- , - (CH 2 ) m -CO- , -CH (R 2 ) -CO-, - (CH 2 ) p -Y-(C(R 3 ) (R 4 )) q -CO-, -NH-CO- or -N(R 5 ) -CO-; in the above-mentioned respective definitions of the X, the bonding arm described at the left end represents a bond with R 1 ; m is an integer of 1 to 3; p is an integer of 0 to 2; q is an integer of 0 to 2; Y: -O- or -SO 2 -; R 2 : phenyl or lower alkyl; R 3 , R 4 : each independently represents hydrogen atom or lower alkyl; R 5 : lower alkyl; provided that the ring portion of the group represented by R 1 is neither naphthylidine nor partially saturated group thereof, and, when X is -CH 2 - or -CO-, R 1 is not naphthyl.
Exploration of a new type of antimalarial compounds based on febrifugine
Kikuchi, Haruhisa,Yamamoto, Keisuke,Horoiwa, Seiko,Hirai, Shingo,Kasahara, Ryota,Hariguchi, Norimitsu,Matsumoto, Makoto,Oshima, Yoshiteru
, p. 4698 - 4706 (2007/10/03)
Febrifugine (1), a quinazoline alkaloid, isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. The use of 1 as an antimalarial drug has been precluded because of side effects, such as diarrhea, vomiting
Method of treating tuberculosis
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Page/Page column 14, (2010/02/10)
Macrolide and ketolides, and compositions containing the same, useful in the treatment of tuberculosis are disclosed. Methods of treating tuberculosis using the macrolides and ketolides, and compositions containing the same, also are disclosed.
Piperidinyl-3-phosphinic acids as novel uptake inhibitors of the neurotransmitter γ-aminobutyric acid (GABA)
Kehler, Jan,Stensbol, Tine B.,Krogsgaard-Larsen, Povl
, p. 811 - 814 (2007/10/03)
Piperidinyl-3-phosphinic acid 2, piperidinyl-3-methylphosphinic acid 3 and N-(4,4-diphenyl-3-butenyl)-piperidinyl-3-phosphinic acid 4 have been synthesized as bioisosteres of the corresponding amino carboxylic acids, which are potent and specific GABA-uptake inhibitors. The novel amino phosphinic acids were tested for their GABA-uptake inhibitory activity and 2 and 4 were identified as the first phosphinic acid based GABA-uptake inhibitors. The methylphosphinic acid 3 was found to be inactive.
