The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
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Paragraph 0993
(2021/03/05)
Preparation method of arylamine o-substituted compound
The invention discloses a preparation method of an arylamine o-substituted compound as shown in a formula I in the specification. The preparation method provided by the invention comprises the following steps: (1) in a continuous flow reactor, carrying ou
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Paragraph 0098-0100
(2019/11/13)
REMOTE HETEROARYL ALKENYLATION WITH CATALYTIC BIFUNCTIONAL TEMPLATE
We report the design of a catalytic, bifunctional template that binds heterocyclic substrate via reversible coordination instead of covalent linkage, allowing remote site- selective C-H olefination of heterocycles. The two metal centers coordinated to this template play different roles; anchoring substrates to the proximity of catalyst and cleaving the remote C-H bonds respectively. Using this strategy, we demonstrate remote site-selective C-H olefination of heterocyclic substrates which do not have functional group handles for covalently attaching templates. For instance the olefination can be an alkenylation of a 3- phenylpyridine with an acrylate alkyl ester selective for the meta position of the phenyl group with respect to the pyridine, or can be an alkenylation of a quinoline with an acrylate alkyl ester selective for the 5-position of the quinoline.
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Page/Page column 23; 24
(2018/09/18)
Palladium-catalyzed annulation of haloanilines and halobenzamides using norbornadiene as an acetylene synthon: A route to functionalized indolines, isoquinolinones, and indoles
A general procedure for the palladium-catalyzed annulation of substituted haloanilines with norbornadiene gives functionalized indolines in 51-98% yield. These indolines can be rapidly converted to benzenoid- substituted indoles and tricyclic indolines. Extension to the use of substituted halobenzamides gives functionalized isoquinolinones in up to 86% yield.
Thansandote, Praew,Hulcoop, David G.,Langer, Michael,Lautens, Mark
supporting information; experimental part
p. 1673 - 1678
(2009/07/17)
Nucleus- and side-chain fluorinated 3-substituted indoles by a suitable combination of organometallic and radical chemistry
Regioselectively fluoro-, trifluoromethyl- and trifluoromethoxy-substituted 3-methyleneindolines have been prepared using a four-step procedure involving metalation/bromination of fluorinated Boc-protected anilines, N-propargylation of the resulting o-bro
Bellezza, Francesca,Cipiciani, Antonio,Ruzziconi, Renzo,Spizzichino, Sara
p. 97 - 107
(2008/12/20)
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