- CRYSTAL FORM I OF A 5-AMINOPYRAZOLE CARBOXAMIDE COMPOUND AS BTK INHIBITOR
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Disclosed is a new crystal form of a 5-aminopyrazole carboxamide compound as shown in Formula (I). Also disclosed are a preparation method for said crystal form of said compound, a pharmaceutical composition of said crystal form of said compound, and uses thereof.
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Paragraph 0036; 0042
(2020/09/23)
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- N-SUBSTITUTED TETRAHYDROTHIENOPYRIDINE DERIVATIVES AND USES THEREOF
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A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection: (I) wherein R1, R2, R3, A, L, m, n, p and q are as defined herein.
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- 5-AMINOPYRAZOLE CARBOXAMIDE DERIVATIVE AS BTK INHIBITOR AND PREPARATION METHOD AND PHARMACEUTICAL COMPOSITION THEREOF
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The present application discloses novel 5-aminopyrazole carboxamide compounds as shown in formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. In addition, the present application further discloses a method for the preparation of the compounds, a pharmaceutical composition comprising a compound of the invention and the use of the compounds.
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Paragraph 0085
(2019/04/16)
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- Mild Metal-Free Hydrosilylation of Secondary Amides to Amines
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The combination of amide activation by Tf2O with B(C6F5)3-catalyzed hydrosilylation with TMDS constitutes a method for the one-pot reduction of secondary amides to amines under mild conditions. The method displays a broad applicability for the reduction of many types of substrates, and shows good compatibility and excellent chemoselectivity for many sensitive functional groups. Reductions of a multifunctionalized α,β-unsaturated amide obtained from another synthetic methodology, and a C-H functionalization product produced the corresponding amines in good to excellent yield. Chemoselective reduction of enantiomeric pure (ee >99%) tetrahydro-5-oxo-2-furaneamides yielded 5-(aminomethyl)dihydrofuran-2(3H)-ones in a racemization-free manner. The latter were converted in one pot to N-protected 5-hydroxypiperidin-2-ones, which are building blocks for the synthesis of many natural products. Further elaboration of an intermediate led to a concise four-step synthesis of -epi-pseudoconhydrine.
- Huang, Pei-Qiang,Lang, Qi-Wei,Wang, Yan-Rong
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p. 4235 - 4243
(2016/06/09)
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- Nonracemic bicyclic lactam lactones via regio- and cis-diastereocontrolled C-H insertion. Asymmetric synthesis of (8S,8aS)-octahydroindolizidin-8-ol and (1S,8aS)-octahydroindolizidin-1-ol
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(Chemical Equation Presented) The Rh2(MPPIM)4- catalyzed intramolecular C-H insertion reaction of (S)- and (R)-1-benzyl-5-(R- diazoacetoxy)piperidin-2-one and (S)-1-benzyl-4-(α-diazoacetoxy) pyrrolidin-2-one proceeds with high regios
- Wee, Andrew G. H.,Fan, Gao-Jun,Bayirinoba, Hypolite M.
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supporting information; experimental part
p. 8261 - 8271
(2010/02/17)
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