130372-07-5Relevant academic research and scientific papers
The use of organophotoacids for deprotection reactions in organic synthesis
Nishikubo, Yuichi,Kanzaki, Shinya,Matsumura, Shuichi,Toshima, Kazunobu
, p. 8125 - 8128 (2006)
o-Hydroxymethylphenol was found to be an effective and environmentally benign organophotoacid. An increased acidity in the excited state, induced by photoirradiation, was sufficient for the deprotection of several protecting groups which are widely used in organic synthesis.
An enantiocontrolled synthesis of (-)-Swainsonine
Kang, Sung Ho,Kim, Geun Tae
, p. 5049 - 5052 (1995)
(-)-Swainsonine 1, first isolated from the fungus Rhizoctonia leguminicola, has been sythesized enantioseletively. The key step was the stereoselective iodoamination of trichloro- acetimidate derived from (Z)- olefinic allylic alcohol 7.
Copper-catalyzed enantioselective synthesis of bridged bicyclic ketals from 1,1-disubstituted-4-methylene-1,6-hexanediols and related alkenols
Burde, Ameya S.,Karyakarte, Shuklendu D.,Sylvester, Eric D.,Chemler, Sherry R.
supporting information, p. 105 - 108 (2021/01/14)
Bridged bicyclic ketals display a range of bioactivities. Their catalytic enantioselective synthesis from acyclic 1,1-disubstituted alkene diols is disclosed. This reaction combines asymmetric catalysis with a distal radical migration. Alkynes and arenes
FUSED TRICYCLIC HETEROCYCLE COMPOUNDS AND THERAPEUTIC USES THEREOF
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Page/Page column 56; 98-99, (2020/01/24)
This application discloses a new class of fused tricyclic heterocycles of formula (I), preparation methods thereof, pharmaceutical compositions comprising these compounds, and pharmaceutically acceptable salts, solvates, or prodrugs thereof, and their use
TRICYCLIC COMPOUNDS AS STING AGONISTS, AND PREPARATION METHODS AND MEDICINAL USES THEREOF
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Page/Page column 55-56; 77-79, (2020/07/07)
Compounds of formula (I) useful as agonists of stimulator of interferon genes (STING), the preparation method therefor, pharmaceutcal compositions comprising the compounds, and the pharmaceutical uses for the treatment of STING-mediated diseases or disord
Intermediate for preparing halichondrin compound and preparation method thereof
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Paragraph 0132; 0156-0159, (2020/07/07)
The invention relates to an intermediate for preparing a halichondrin compound and a preparation method thereof. The invention particularly relates to an intermediate for preparing halichondrin, eribulin or analogues thereof, and a preparation method and application of the intermediate. The intermediate as well as the preparation method and application thereof are used for constructing C20-C26 structural fragments of the halichondrin compound. The initial raw materials of the synthesis route are cheap, easy to obtain, stable in source and reliable in quality; the structural characteristics ofreactants are fully utilized in the selection of a chiral center construction method, so that the synthesis efficiency is practically improved, and the difficulty and risk of product quality control are reduced; and the use of a high-toxicity and expensive organic tin catalyst is avoided, so that the cost and the environmental friendliness are remarkably improved.
DNA sequencing reaction additive
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Page/Page column 93; 94; 105, (2020/12/07)
The present invention provides methods, compositions, mixtures and kits utilizing 5-Chloro-2-methyl-4-isothiazolin-3-one in sequencing reactions, and in particular, sequencing reactions where deoxynucleoside triphosphates comprising a 3′-O position capped
PYRROLIDINE DERIVATIVE
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Paragraph 0433, (2019/04/16)
The present invention aims to provide a novel compound which has CGRP receptor antagonist activity and which is useful for the treatment of various diseases mediated by CGRP receptors. That is, the present invention relates to the pyrrolidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. In the formulae, W is ring, X is a carbon atom or the like, Y1 to Y4 are carbon atoms or the like, and R1 to R7 is alkyl or the like. The compounds of the present invention or a pharmaceutically acceptable salt thereof have an excellent CGRP receptor antagonist activity, and thus are useful as agents for the treatment of various diseases mediated by CGRP receptors.
Introduction of Cyclopropyl and Cyclobutyl Ring on Alkyl Iodides through Cobalt-Catalyzed Cross-Coupling
Andersen, Claire,Ferey, Vincent,Daumas, Marc,Bernardelli, Patrick,Guérinot, Amandine,Cossy, Janine
supporting information, p. 2285 - 2289 (2019/03/29)
A cobalt-catalyzed cross-coupling between alkyl iodides and cyclopropyl, cyclobutyl, and alkenyl Grignard reagents is disclosed. The reaction allows the introduction of strained rings on a large panel of primary and secondary alkyl iodides. The catalytic system is simple and nonexpensive, and the reaction is general, chemoselective, and diastereoconvergent. The alkene resulting from the cross-coupling can be transformed to substituted cyclopropanes using a Simmons-Smith reaction. The formation of radical intermediates during the coupling is hypothesized.
Chemoselective deoxygenation of ether-substituted alcohols and carbonyl compounds by B(C6F5)3-catalyzed reduction with (HMe2SiCH2)2
Yang, Wenyu,Gao, Lu,Lu, Ji,Song, Zhenlei
supporting information, p. 4834 - 4837 (2018/05/23)
B(C6F5)3-catalyzed deoxygenation of ether-substituted alcohols and carbonyl compounds has been developed using (HMe2SiCH2)2 as the reductant. This unique reagent shows distinct superiority over traditional one silicon-centered hydrosilanes, giving the corresponding alkanes in high yields with good tolerance of ethers, aryl halides and alkenes. The control experiments suggest that (HMe2SiCH2)2 might facilitate the approach in an intramolecular Si/O activation manner.
