- Phase transfer alkylation of arylacetonitriles revisited
-
Phase transfer alkylations of phenylacetonitrile derivatives carried out in the presence of 60-75% aqueous KOH, instead of the typical 50% NaOH, provide substantial improvements in the overall yields and purity of products. Reactions with simple secondary alkyl halides, as well as cycloalkylations with 1,2- and 1,3-dihaloalkanes proceed with good yields. Increasing the concentration of base diminishes the formation of by-products from competitive β-elimination processes.
- Barbasiewicz, Micha?,Marciniak, Karolina,Fedoryński, Micha?
-
-
Read Online
- Amide compound and derivative thereof, preparation method, pharmaceutical composition and application thereof
-
The invention discloses an amide compound and derivative thereof, a preparation method, a pharmaceutical composition and application thereof. The structure of the amide compound is shown as a formula (I). The derivatives of theamide compound relate to a stereoisomer, a tautomer, a metabolite, a metabolic precursor, a prodrug, a solvate, a salt of the solvate, a crystal, a pharmaceutically acceptable salt or a mixture of the above of theamide compound. The amide compound and the derivative thereof have an efficient inhibition effect on indoleamine 2, 3-dioxygenase 1, and can be used for preparing medicines for treating indoleamine 2, 3-dioxygenase 1 mediated immunosuppression related diseases, the prepared medicine can exert the medicine effect at the molecular level and is wide in application, and the synthesis method of the compound is simple, convenient and easy to operate.
- -
-
Paragraph 0390-0393
(2021/07/09)
-
- Iridium-Catalyzed Enantioselective C(sp3)–H Borylation of Cyclobutanes
-
We herein report the first example of iridium-catalyzed enantioselective C(sp3)–H borylation of cyclobutanes using benzoxazoline as the directing group. The combination of a chiral bidentate boryl ligand and an iridium precursor has found to effectively catalyze C(sp3)–H borylation to afford a variety of cyclobutylboronates with good to excellent enantioselectivities. We also demonstrate the synthetic utility of the current method by converting the stereogenic C—B bond to other functionalities.
- Chen, Xiang,Chen, Lili,Zhao, Hongliang,Gao, Qian,Shen, Zhenlu,Xu, Senmiao
-
supporting information
p. 1533 - 1537
(2020/09/09)
-
- HETEROCYCLIC COMPOUND
-
The problem of the present invention is to provide a compound having a PDE2A inhibitory action, and useful as a prophylactic or therapeutic drug for schizophrenia, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
- -
-
Paragraph 0664
(2016/09/26)
-
- Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)
-
N-(5-Chloro-2,4-dihydroxyphenyl)-1-phenylcyclobutanecarboxamide (N-CDPCB, 1a) is found to be an inhibitor of the fat mass and obesity associated protein (FTO). The crystal structure of human FTO with 1a reveals a novel binding site for the FTO inhibitor and defines the molecular basis for recognition by FTO of the inhibitor. The identification of the new binding site offers new opportunities for further development of selective and potent inhibitors of FTO, which is expected to provide information concerning novel therapeutic targets for treatment of obesity or obesity-associated diseases.
- He, Wu,Zhou, Bin,Liu, Weijia,Zhang, Meizi,Shen, Zhenhua,Han, Zhifu,Jiang, Qingwei,Yang, Qinghua,Song, Chuanjun,Wang, Ruiyong,Niu, Tianhui,Han, Shengna,Zhang, Lirong,Wu, Jie,Guo, Feima,Zhao, Renbin,Yu, Wenquan,Chai, Jijie,Chang, Junbiao
-
p. 7341 - 7348
(2015/10/05)
-
- PROCESS OF PREPARING 3-(3-(4-(1-AMINOCYCLOBUTYL)PHENYL)-5-PHENYL-3H-IMIDAZO[4,5-B]PYRIDIN-2-YL)PYRIDIN-2-AMINE
-
The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:
- -
-
Paragraph 0160; 0161
(2015/11/03)
-
- Cycloalkyl Amine Compounds
-
Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C═O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
- -
-
Paragraph 0247; 0248
(2015/03/04)
-
- Fe-catalyzed regiodivergent [1,2]-shift of α-aryl aldehydes
-
An Fe-catalyzed conversion of aldehydes to ketones via [1,2]-shift has been developed. This skeletal rearrangement shows a wide substrate scope and chemoselectivity profile while exhibiting an excellent [1,2]-aryl or [1,2]-alkyl shift selectivity that is easily switched by electronic effects.
- Gutierrez-Bonet, Alvaro,Flores-Gaspar, Areli,Martin, Ruben
-
supporting information
p. 12576 - 12579
(2013/09/23)
-
- PYRAZOLE DERIVATIVES AS MODULATORS OF CALCIUM RELEASE -ACTIVATED CALCIUM CHANNEL
-
Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
- -
-
Page/Page column 71
(2011/04/26)
-
- IL-8 RECEPTOR ANTAGONISTS
-
This invention relates to novel compounds, compositions and combinations thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
- -
-
Page/Page column 52
(2008/12/06)
-
- A polar substituent effect on the ring-cleavage rearrangement of 1-arylcyclobutylmethyl Grignard reagents
-
The kinetics of the ring-cleavage rearrangements of 1-phenylcyclobutylmethylmagnesium chloride and its p-methyl and p-chloro analogs have been determined.The first-order rate constants are correlated by the Hammett equation, with ρ=-0.47.The results are consistent with a concerted mechanism with a cyclic transition state having significant polar character, although polar effects on the stabilities of reactant and product may also contribute.The phenyl group itself slows the reaction by a factor of 0.031, which is interpreted principally in terms of steric destabilization of the transition state.
- Hill, E. Alexander,Li, Baoju
-
-
- CATHODIC SYNTHESIS OF CYCLOBUTANES
-
Cathodic electrolysis of compounds with an activated methylene group in the presence of 1,3-dibromopropane affords 1,1-disubstituted cyclobutanes.
- Vasil'ev, A. A.,Tatarinova, V. I.,Petrosyan, V. A.
-
p. 1221 - 1224
(2007/10/02)
-