87727-28-4Relevant articles and documents
Stereoselective synthesis of the chiral tetrahydropyrane core of swinholides and misakinolides
Hayakawa, Hiroyuki,Iida, Kouki,Miyazawa, Masahiro,Miyashita, Masaaki
, p. 601 - 602 (1999)
Stereoselective synthesis of the optically pure tetrahydropyrane core of swinholides and misakinolide A starting from (S)-methyl lactate is described in which the highly stereoselective intramolecular iodoetherification for construction of the tetrahydropyrane ring and the regioselective ring-opening reaction of an epoxide are involved as key steps.
Catalytic Macrocyclization Strategies Using Continuous Flow: Formal Total Synthesis of Ivorenolide A
De Léséleuc, Mylène,Godin, éric,Parisien-Collette, Shawn,Lévesque, Alexandre,Collins, Shawn K.
, p. 6750 - 6756 (2016)
A formal total synthesis of ivorenolide A has been accomplished employing a Z-selective olefin cross metathesis and a macrocyclic Glaser-Hay coupling as key steps. The macrocyclization protocol employed a phase separation/continuous flow manifold whose ad
Pyrimidine-4 (3H)-ketone heterocyclic compound, preparation method thereof and application of pyrimidine-4 (3H)-ketone heterocyclic compound in medicine
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Paragraph 0401-0403; 0408-0411, (2021/07/21)
The invention relates to pyrimidine-4 (3H)-ketone heterocyclic compounds suitable for inhibiting or regulating SHP2, a preparation method of the pyrimidine-4 (3H)-ketone heterocyclic compounds and application of the pyrimidine-4 (3H)-ketone heterocyclic compounds in medicine. Specifically, the invention relates to a compound as shown in a general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, a method for treating and/or preventing related diseases mediated by SHP2, especially cancers by using the compound or the pharmaceutically acceptable salt thereof, and a preparation method of the compound or the pharmaceutically acceptable salt thereof. The invention also relates to application of the compound or the pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof in preparation of drugs for treating and/or preventing SHP2-mediated related diseases. Wherein each substituent in the general formula (I) is as defined in the specification.
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders
Yang, Xiangbo,Wang, Zhijia,Pei, Yuan,Song, Ning,Xu, Lei,Feng, Bo,Wang, Hanlin,Luo, Xiaomin,Hu, Xiaobei,Qiu, Xiaohui,Feng, Huijin,Yang, Yaxi,Zhou, Yubo,Li, Jia,Zhou, Bing
, (2021/04/02)
SHP2, a non-receptor tyrosine phosphatase, plays a pivotal role in numerous oncogenic cell-signaling cascades like RAS-ERK, PI3K-AKT and JAK-STAT. On the other hand, proteolysis targeting chimera (PROTAC) has emerged as a promising strategy for the degrad
Structure–activity relationship study of the anti-obesity natural product yoshinone A
Kawazoe, Yoshinori,Itakura, Yuki,Inuzuka, Toshiyasu,Omura, Sachikazu,Uemura, Daisuke
, p. 226 - 232 (2021/03/06)
Yoshinone A was derived from marine algae and shown to inhibit adipogenic differentiation. The natural compound is composed of a γ-pyrone ring and a side chain and that contains two asymmetric carbons. Although their absolute configuration has been determ
SHP2 INHIBITORS AND USES THEREOF
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Page/Page column 133; 134, (2021/04/02)
Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.
PYRIMIDINE-FUSED CYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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Paragraph 0380; 0383-0385; 0889-0890, (2021/02/26)
Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.
A Unified Strategy for the Asymmetric Synthesis of Highly Substituted 1,2-Amino Alcohols Leading to Highly Substituted Bisoxazoline Ligands
Shrestha, Bijay,Rose, Brennan T.,Olen, Casey L.,Roth, Aaron,Kwong, Adon C.,Wang, Yang,Denmark, Scott E.
, p. 3490 - 3534 (2021/02/16)
A general procedure for the asymmetric synthesis of highly substituted 1,2-amino alcohols in high yield and diastereoselectivity is described that uses organometallic additions of a wide range of nucleophiles to tert-butylsulfinimines as the key step. The addition of organolithium reagents to these imines follows a modified Davis model. The diastereoselectivity for this reaction depends significantly on both the nucleophile and electrophile. These highly substituted 1,2-amino alcohols are used to synthesize stereochemically diverse and structurally novel, polysubstituted 2,2′-methylene(bisoxazoline) ligands in high yields.
PYRAZOLO[3,4-B]PYRAZINE SHP2 PHOSPHATASE INHIBITORS
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Page/Page column 127, (2021/02/26)
The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising sa
PROCESS OF MANUFACTURE OF A COMPOUND FOR INHIBITING THE ACTIVITY OF SHP2
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, (2020/05/12)
The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II wit
