138036-92-7Relevant academic research and scientific papers
Molybdenum pentachloride (MoCl5) or molybdenum dichloride dioxide (MoO2Cl2): advanced catalysts for thioacetalization of heterocyclic, aromatic and aliphatic compounds
Goswami, Shyamaprosad,Maity, Annada C.
, p. 3092 - 3096 (2008)
A new, convenient and mild method for thioacetalization of heterocyclic, aromatic and aliphatic compounds catalyzed by MoCl5 or MoO2Cl2 is described. This novel method is important for the synthesis of the difficult to prepare heterocyclic thioacetals such as the pterin thioacetals and it offers significant advantages such as high conversion, short reaction times and simplicity in operation.
SHP2 PHOSPHATASE INHIBITORS AND METHODS OF MAKING AND USING THE SAME
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Paragraph 0177-0178, (2021/04/02)
The disclosure is in part directed to crystalline forms of (R)-1′-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4′-piperidin]-3-amine, its salt, and variants thereof.
Compound serving as SHP2 inhibitor and application thereof
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Paragraph 0191; 0193-0195, (2021/05/12)
The invention belongs to the field of medical chemistry, relates to a compound serving as an SHP2 inhibitor and an application of the compound, and particularly provides a compound shown in a formula (I) or an isomer, pharmaceutically acceptable salt, solvate, crystal or prodrug of the compound, processes for the preparation, pharmaceutical compositions containing these compounds and the use of these compounds or compositions for the treatment of SHP2 mediated diseases.
CARBOXAMIDE-PYRIMIDINE DERIVATIVES AS SHP2 ANTAGONISTS
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Page/Page column 120, (2020/09/19)
The invention relates to carboxamide-pyrimidine derivatives of the general formula (I), or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in
SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Paragraph 0212; 0299, (2019/10/15)
The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
Synthesis of Chiral α-Aminosilanes through Palladium-Catalyzed Asymmetric Hydrogenation of Silylimines
Fan, Dongyang,Liu, Yang,Jia, Jia,Zhang, Zhenfeng,Liu, Yangang,Zhang, Wanbin
supporting information, p. 1042 - 1045 (2019/05/16)
The asymmetric hydrogenation of silylimines was first developed by using a palladium complex of a P-stereogenic diphosphine ligand as the catalyst, affording the valuable chiral α-aminosilanes with quantitative conversions and excellent enantioselectiviti
A 2 - substituted - 1, 3 - dithiane derivative of the preparation method
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Paragraph 0023; 0024; 0025; 0026; 0027, (2019/06/26)
The invention provides a preparation method of a 2-substituted-1,3-dithiane derivative. The preparation method comprises the following steps: adding 1,3-dithiane (CAS:505-23-7) and 1,2-dichloroethane (DCE) or dichloromethane (DCM) into a reaction bottle, adding N-chlorosuccinimide (NCS) under ice-bath condition, and stirring for 0.5-1 h to prepare a 2-chloro-1,3-dithiane solution; and adding an aldehyde or ketone compound and a lewis acid catalyst into the above solution, and reacting to prepare the 2-substituted-1,3-dithiane derivative. By using the 1,3-dithiane solid and different types of aldehyde and keto-carbonyl compounds as raw material and using one or more of ferric trichloride, boron trifluoride diethyl etherate, methanesulfonic acid, aluminum trichloride, ferrous chloride and nickel chloride as catalysts, preparation of the 2-substituted-1,3-dithiane derivative is realized. The catalysts used in the invention are cheap and easily available, dosage of the catalysts is low and pollution of the catalysts is little. The solid raw materials used in the invention can avoid use of fetid toxic 1,3-dimercaptopropane with strong volatility, and the purpose of protecting an experimenter's body and reducing environmental pollution is realized. In addition, the preparation method has advantages of mild reaction condition, high yield, simple operation and the like.
Sulfur-Directed Ligand-Free C-H Borylation by Iridium Catalysis
Liu, Li,Wang, Guanghui,Jiao, Jiao,Li, Pengfei
supporting information, p. 6132 - 6135 (2017/11/24)
An iridium-catalyzed ortho C-H borylation reaction directed by cyclic dithioacetal moiety is disclosed. A series of borylation products were obtained in moderate to good yields under mild conditions in exclusive mono- and ortho-regioselectivity. Thus, the 1,3-dithiane or 1,3-dithiolane group serves as a remarkable effective directing group for C-H borylation without any ligand assistance. The further transformations of the borylation products are also carried out to change boryl group to other functional groups.
Fe-catalyzed direct dithioacetalization of aldehydes with 2-chloro-1,3-dithiane
Lai, Junshan,Du, Wenbin,Tian, Lixia,Zhao, Changgui,She, Xuegong,Tang, Shouchu
, p. 4396 - 4399 (2015/01/08)
Present methods to synthesize 1,3-dithiane molecules require either harsh reaction conditions or highly specialized reagents. We have developed a catalytic dithioacetalization process that directly gains access to the corresponding 1,3-dithianes using aldehydes and 2-chloro-1,3-dithiane in a highly efficient manner. This methodology is beneficial due to mildness of the reaction conditions, and the dithioacetaliation process results in good to excellent yields by using 15 mol % of an iron catalyst.
Reversed-polarity synthesis of Diaryl Ketones through palladium-catalyzed direct Arylation of 2-Aryl-1,3-dithianes
Yucel, Baris,Walsh, Patrick J.
supporting information, p. 3659 - 3667 (2015/01/09)
An umpolung approach to the synthesis of diaryl ketones has been developed based on in situ generation of acyl anion equivalents and their catalytic arylation. This method entails the base-promoted, palladium-catalyzed direct C-H arylation of 2- aryl-1,3-dithianes with aryl bromides. Use of MNACHTUNGTRENUNG( SiMe3)2 (M=Li, Na) base results in reversible deprotonation of the weakly acidic dithiane. In the presence of a Pd(NiXantphos)-based catalyst and aryl bromide, cross-coupling of the metallated 2-aryl- 1,3-dithiane takes place under mild conditions (2 h at rt) with yields as high as 96%. The resulting 2,2- diaryl-1,3-dithianes were converted into diaryl ketones by either molecular iodine, N-bromo succinimide (NBS) or Selectfluor in the presence of water. The dithiane arylation/hydrolysis can be performed in a one-pot procedure to yield a variety of diaryl ketones in good to excellent yields. This method is suitable for rapid and large-scale synthesis of diaryl ketones. A one-pot preparation of anti-cholesterol drug fenofibrate (TriCor) has been achieved on 10.0 mmol scale in 86% yield.
