124276-83-1Relevant academic research and scientific papers
Preparation method of arylcyclopropane compound
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Paragraph 0023-0028; 0074-0078, (2022/01/10)
The present invention discloses a method for preparing an arylcyclopropane compound, 1.0eq phenylacetonitrile and 1.1eq 1-bromo-2-chloroethane as the starting material, N, N- dimethylacetamide as a solvent, solvent dosage of 10V, plus 2.5eq sodium hydride
Nickel-Catalyzed Favorskii-Type Rearrangement of Cyclobutanone Oxime Esters to Cyclopropanecarbonitriles
Shuai, Bin,Fang, Ping,Mei, Tian-Sheng
, p. 1637 - 1641 (2021/10/02)
A nickel-catalyzed base-promoted rearrangement of cyclobutanone oxime esters to cyclopropanecarbonitriles was developed. The ring opening of cyclobutanone oxime esters occurs at the sterically less hindered side. A base-promoted nickelacyclobutane intermediate, formed in situ, is assumed to be involved in the formation of the product.
Chiral Bidentate Boryl Ligand Enabled Iridium-Catalyzed Enantioselective C(sp3)-H Borylation of Cyclopropanes
Shi, Yongjia,Gao, Qian,Xu, Senmiao
supporting information, p. 10599 - 10604 (2019/08/28)
We herein report an Ir-catalyzed enantioselective C(sp3)-H borylation of cyclopropanecarboxamides using a chiral bidentate boryl ligand for the first time. A variety of substrates with α-quaternary carbon centers could be compatible in this reaction to provide β-borylated products with good to excellent enantioselectivities. We have also demonstrated that the borylated products can be used as versatile precursors engaging in stereospecific transformations of C-B bonds, including the synthesis of a bioactive compound Levomilnacipran.
PD(II)-CATALYZED ENANTIOSELECTIVE C-H ARYLATION OF FREE CARBOXYLIC ACIDS
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Page/Page column 26, (2019/11/12)
The invention includes procedures for stereoselective β-arylation of carboxylic acids having a β-carbon atom. For example, stereoselective arylation procedures include the following reactions: (I)
A NOVEL PROCESS FOR THE SYNTHESIS OF 1-ARYL-1-TRIFLUOROMETHYLCYCLOPROPANES
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Page/Page column 19; 20, (2018/08/26)
The present invention relates to a process for the manufacturing of 1-aryl-1-trifluoromethylcyclopropanes, which serve as intermediates for the manufacturing of calcium T channel blockers of the general formula (A) which are described in WO 2015/186056.
Pd(II)-Catalyzed Enantioselective C(sp3)-H Arylation of Free Carboxylic Acids
Shen, Peng-Xiang,Hu, Liang,Shao, Qian,Hong, Kai,Yu, Jin-Quan
supporting information, p. 6545 - 6549 (2018/05/23)
A monoprotected aminoethyl amine chiral ligand based on an ethylenediamine backbone was developed to achieve Pd-catalyzed enantioselective C(sp3)-H arylation of cyclopropanecarboxylic and 2-aminoisobutyric acids without using exogenous directing groups. This new chiral catalyst affords new disconnection for preparing diverse chiral carboxylic acids from simple starting materials that are complementary to the various ring forming approaches.
Rhodium-Catalyzed Enantioselective Silylation of Cyclopropyl C?H Bonds
Lee, Taegyo,Hartwig, John F.
supporting information, p. 8723 - 8727 (2016/07/21)
Hydrosilyl ethers, generated in situ by the dehydrogenative silylation of cyclopropylmethanols with diethylsilane, undergo asymmetric, intramolecular silylation of cyclopropyl C?H bonds in high yields and with high enantiomeric excesses in the presence of
Meta-selective C-H functionalization using a nitrile-based directing group and cleavable Si-tether
Lee, Sunggi,Lee, Hyelee,Tan, Kian L.
supporting information, p. 18778 - 18781 (2014/01/06)
A nitrile-based template that enables meta-selective C-H bond functionalization was developed. The template is applicable to a range of substituted arenes and tolerates a variety of functional groups. The directing group uses a silicon atom for attachment
NOVEL INDOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON I B KINASE
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Page/Page column 34-35, (2009/12/05)
Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKKβ and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKKβ. In the formula, R1 represents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; R2 represents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like.
CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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Page/Page column 61-62, (2010/02/11)
This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of G, E, E, n, R1, R2, R3 et R4 are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
