185099-67-6Relevant articles and documents
Retro-aza-Michael reaction in continuous flow. Approaches to synthesis of adaline and euphococcinine related products
Sienkiewicz, Michal,Pawelski, Damian,Podgorska, Katarzyna,Lazny, Ryszard
, (2022/03/07)
A retro-aza-Michael ring opening reaction of tropinone and granatanone (pseudopelletierine) in flow setup was investigated and the resulting products were utilized as key intermediates in approaches to adaline and its analogues. The enantioselective flow-reaction gave products of ring opening of granatanone with enantiopurity up to 98% ee. Attempts to elaborate the retro-aza-Michael product to alkaloids are described. Lithiated carbamate derivative of tropane was converted to a tropane analogue of euphococcinine, an adaline related alkaloid (a methyl and tropane homologue of adaline 19). Reactivity of the retro-aza-Michael product under Morita-Baylis-Hillman conditions was also briefly investigated.
METHODS AND COMPOSITIONS FOR MODULATING SPLICING
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Paragraph 01005, (2020/08/22)
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
Decarboxylative Oxygenation via Photoredox Catalysis
Faraggi, Tomer M.,Li, Wei,MacMillan, David W. C.
, p. 410 - 415 (2019/12/24)
The direct conversion of aliphatic carboxylic acids to their dehomologated carbonyl analogues has been accomplished through photocatalytic decarboxylative oxygenation. This transformation is applicable to an array of carboxylic acid motifs, producing ketones, aldehydes, and amides in excellent yields. Preliminary results demonstrate that this methodology is further amenable to aldehyde substrates via in situ oxidation to the corresponding acid and subsequent decarboxylative oxygenation. We have exploited this strategy for the sequential oxidative dehomologation of linear aliphatic chains.
Tropane alkaloid compounds and method of manufacturing using sequential oxidation reactions
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, (2020/06/16)
The present invention relates to a tropane alkaloid compound sequentially using an oxidative Mannich ring reaction and a method for producing the same. The present invention provides a tropane alkaloid compound having a structure of chemical formula 1 in
CHROMEN-4-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS DISEASE
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Page/Page column 80, (2020/05/21)
The present invention provides novel compounds having the general formula (I) wherein R1 to R6, and m are as described herein, compositions including the compounds and methods of using the compounds.
Compound and application thereof
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Paragraph 0245-0248, (2019/04/17)
The invention provides a novel compound. The novel compound has certain inhibitory activity for indoleamine 2,3-dioxygenase (IDO) which is oxido-reductase, and accordingly the novel compound can be used for treating diseases related to the indoleamine 2,3-dioxygenase and can be applied to cancer and immunity related diseases.
Construction of 8-Azabicyclo[3.2.1]octanes via Sequential DDQ-Mediated Oxidative Mannich Reactions of N-Aryl Pyrrolidines
Jo, Hanbyeol,Hassan, Ahmed H. E.,Jung, Seung Young,Lee, Jae Kyun,Cho, Yong Seo,Min, Sun-Joon
, p. 1175 - 1178 (2018/02/23)
A concise synthesis of 8-azabicyclo[3.2.1]octanes via sequential oxidative Mannich reactions is described. This approach involves an intermolecular oxidative Mannich coupling reaction between N-aryl pyrrolidines with TMS enol ether and a subsequent intramolecular oxidative Mannich cyclization of the corresponding silyl enol ether. DDQ is used as a key oxidant for both reactions.
CDK kinase inhibitors
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Paragraph 0417; 0419-0421, (2017/08/02)
The present invention belongs to the technical field of medicine, and particularly relates to a CDK kinase inhibitor represented by a general formula (I), a pharmaceutically acceptable salt of the CDK kinase inhibitor, an ester of the CDK kinase inhibitor, a solvate of the CDK kinase inhibitor and stereoisomers of the CDK kinase inhibitor, the pharmaceutically acceptable salt, the ester and the solvate, wherein R1, R2, R3, R4, R5 and n are defined in the specification. The present invention further relates to preparation methods of the compounds, pharmaceutical formulations containing the compounds, pharmaceutical compositions containing the compounds, and applications of the compound, the pharmaceutically acceptable salt, the ester, the solvate and the stereoisomers in preparation of treatment and/or preparation of CDK kinase-mediated cancer associated diseases. The formula (I) is defined in the specification.
Tyrosine Kinase Inhibitor And Uses Thereof
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Paragraph 0516-0517, (2017/05/15)
Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
7H-Pyrrolo[2,3-d]pyrimidine-4-thiol derivatives using as JAK-3 inhibitors
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Paragraph 0139-0141, (2017/10/21)
The present invention relates to a method for preparing a novel 7H-pyrrolo[2,3-d]pyrimidine-4-thiol derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient. The composition containing the novel 7H-pyrrolo[2,3-d]pyrimidine-4-thiol derivative according to the present invention can be useful for preventing or treating diseases caused by the overactivity of a Janus kinase (JAK).