121959-61-3Relevant articles and documents
Insulin-like growth factor-1 receptor tyrosine kinase inhibitor and uses thereof
-
Paragraph 0062; 0065-0067, (2020/01/25)
The invention discloses a class of compounds capable of being used as an insulin-like growth factor-1 receptor tyrosine kinase inhibitor, and a preparation method thereof, a pharmaceutical compositioncontaining the compound, and applications of the pharma
Novel small molecule inhibitor of insulin-like growth factor-1 receptor and application of novel small molecule inhibitor
-
Paragraph 0046-0049, (2021/01/04)
The invention provides a novel small-molecule inhibitor of an insulin-like growth factor 1 receptor and application of the novel small-molecule inhibitor. The novel small-molecule inhibitor is a derivative of picropodophyllotoxin; fluorine atoms are used for replacing hydrogen atoms at two positions of the left side of picropodophyllotoxin, so that the capacity of molecules penetrating through a blood-brain barrier is improved; meanwhile, deuterium atoms are used for replacing hydrogen atoms, so that the half-life period of the molecules in an organism can be effectively prolonged. The small-molecule inhibitor can be used for preparing drugs for preventing and treating cancers. Compared with picropodophyllotoxin in the clinical test stage at present, the small-molecule inhibitor has higherblood-brain barrier permeability and longer in-vivo half-life while maintaining the action mechanism and biochemical characteristics of picropodophyllotoxin. When used alone, the small-molecule inhibitor can effectively inhibit proliferation and brain metastasis of various tumors, and can be synergistically combined with other anti-cancer drugs, so that proliferation of tumor cells is efficientlyinhibited, and the lifetime is remarkably prolonged.
Improved Synthesis of Racemate and Enantiomers of Taniguchi Lactone and Conversion of Their C-C Double Bonds into Triple Bonds
Malová Kri?ková, Petra,Lindner, Wolfgang,Hammerschmidt, Friedrich
, p. 651 - 657 (2017/11/15)
cis -2-Butene-1,4-diol was heated with triethyl orthoacetate and p -hydroquinone as catalyst at 170 °C to give racemic Taniguchi lactone. It was converted into diastereomeric amides with (S)-1-phenylethylamine for stereoisomer resolution. The double bonds
METHOD FOR PRODUCING LACTONE COMPOUND
-
Paragraph 0033; 0035, (2019/01/04)
PROBLEM TO BE SOLVED: To provide a method that makes it possible to efficiently produce a lactone compound in a short process from a raw material that is inexpensive and easily available. SOLUTION: The present invention provides a method for producing a lactone compound by the reaction between a diester compound and orthocarboxylate, in the presence of a Lewis acid catalyst; preferably, the Lewis acid is a metal compound; preferably, a ligand of the Lewis acid is an alkyl group, an alkoxy group, a carboxy group or an acetyl acetone; the Lewis acid is dialkyltin oxide. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
Facile production scale synthesis of (S)-Taniguchi lactone: A precious building-block
Von Kieseritzky, Fredrik,Wang, Yeliu,Axelson, Magnus
, p. 643 - 645 (2014/06/09)
A cost-efficient and facile synthesis of (S)-4-vinyldihydrofuran-2(3H)-one ((S)-1), better known as (S)-Taniguchi lactone, is described. Racemic Taniguchi lactone rac-1 was ring-opened with (S)-1-benzylmethylamine providing a diastereomeric mixture of hyd
Asymmetric total syntheses of (-)-penicipyrone and (-)-tenuipyrone via biomimetic cascade intermolecular michael addition/cycloketalization
Song, Liyan,Yao, Hongliang,Zhu, Liangyu,Tong, Rongbiao
supporting information, p. 6 - 9 (2013/03/28)
The first total syntheses of (-)-penicipyrone and (-)-tenuipyrone were accomplished enantioselectively in 12 steps with an 11% yield and 6 steps with a 28% yield from the known 4-((tert-butyldimethylsilyl)oxy)-cyclopent-2-enone, respectively, by developing a biomimetic bimolecular cascade cyclization featuring an intermolecular Michael addition/cyclo-(spiro-)ketalization sequence. The relative, absolute stereochemistry and carbon connectivity of penicipyrone was further confirmed by X-ray crystallographic analysis and comparison of optical rotations.
Enantioselective Iridium-catalyzed allylic alkylations - Improvements and applications based on salt-free reaction conditions
Gnamm, Christian,F?rster, Sebastian,Miller, Nicole,Br?dner, Kerstin,Helmchen, Günter
, p. 790 - 794 (2007/12/29)
Simplified procedures for the Ir-catalyzed asymmetric allylic alkylation reaction are described that often allow substitution products to be obtained with ≥99% ee. Applications to syntheses of important chiral building blocks, such as the Taniguchi lacton
Highly stereoselective radical cyclization of haloacetals controlled by the acetal center
Villar, Felix,Kolly-Kovac, Tanja,Equey, Olivier,Renaud, Philippe
, p. 1566 - 1577 (2007/10/03)
A systematic investigation of radical haloacetal cyclizations (Ueno-Stork reaction) where the acetal center is the unique stereogenic element is reported. This highly diastereoselective reaction can be used for the preparation of polysubstituted tetrahydrofurans and γ-lactones. We report herein the full experimental details of reactions where up to three new chiral centers are created. To demonstrate the potential of this approach, short syntheses of (+)-eldanolide and of tricyclic acetals related to biologically active lignans have been achieved.
Radical cyclization on solid support: Synthesis of γ-butyrolactones
Watanabe, Yoshihiko,Ishikawa, Satoshi,Takao, Gou,Toru, Takeshi
, p. 3411 - 3414 (2007/10/03)
Synthesis of γ-butyrolactones using radical cyclization on solid-phase has been achieved. Polymer-supported β-bromoethylacetals were treated with tributyltin hydride in the presence of a catalytic amount of α,α'- azobisisobutyronitrile to generate intermediate carbon radicals which cyclize onto the intramolecular carbon-carbon double bond. The cyclization products were released by Jones oxidation from resin to give γ-butyrolactones in good yields.
Synthesis and absolute configuration of the insecticidal sesquilignan ( + )-haedoxan a in honour of professor G. H. Neil towers 75th birthday
Ishibashi, Fumito,Taniguchi, Eiji
, p. 613 - 622 (2007/10/03)
The insecticidal neolignan, ( + )-haedoxan A, was synthesized from (S)-( + )-vinyl-y-butyrolactone and (2R,3R)-(+)-6-formyl-7-methoxy-3-methoxymethyl-2-(3,4-methylenedioxyphenyl)-1,4- benzodioxane, and its absolute configuration was unequivocally establis