62420-83-1

Upstream product

• 245-43-2 benzo<2,3>indolizine 
• 71-41-0 pentan-1-ol 
• 138344-24-8 2-(4-chlorobutyl)-1H-indole 
• 46169-71-5 1-(but-3-en-1-yl)-1H-indole 
• 156237-68-2 1-(4-iodobutyl)-1H-indole 
• 1575-61-7 5-Chlorovaleroyl chloride 
• 138344-23-7 2-(4-Chloro-butyl)-indole-1-carboxylic acid tert-butyl ester 
• 138344-22-6 [2-(6-Chloro-2-oxo-hexyl)-phenyl]-carbamic acid tert-butyl ester 
• 120-72-9 indole 
• 1054668-39-1 6-(1H-indol-1-yl)hexan-2-one 
• 148317-65-1 1-(4-Bromobutyl)-2-<(4-methylphenyl)sulfonyl>-1H-indole 
• 148317-68-4 1-(4-Iodobutyl)-2-<(4-methylphenyl)sulfonyl>-1H-indole 
• 131849-07-5 7,8-dihydropyrido<1,2-a>indol-9(6H)-one 
• 106392-60-3 1-(4-bromobutyl)-1H-indole 

Relevant academic research and scientific papers

A Dieckmann/ring expansion approach to tetrahydropyrido- and tetrahydroazepino-[1,2-a]indoles

A general Dieckmann/ring expansion approach to fused[1,2-a]indole systems is reported. This approach has allowed the synthesis of a large variety of substituted systems required for the preparation of a series of potent and selective inhibitors of Protein Kinase C.

Nickel-catalyzed, ring-forming aromatic C–H alkylations with unactivated alkyl halides

The development of a nickel-catalyzed C–H alkylation of aromatic substrates with unactivated alkyl halides is described. This carbocyclization facilitates the synthesis of diverse fused ring systems from simple aromatic substrates and is an attractive alt

AMINOPYRIMIDINE COMPOUNDS, PREPARATION METHODS AND USES THEREOF

Provided herein are novel compounds, for example, compounds having a Formula (I) or Formula (II), or a pharmaceutically acceptable salt thereof. Also provided herein are methods of preparing the compounds and methods of using the compounds, for example, for treating various cancer described herein, such as lung cancer (e.g., non-small cell lung cancer).

Deacylation-aided C–H alkylative annulation through C–C cleavage of unstrained ketones

Arene- and heteroarene-fused rings are pervasive in biologically active molecules. Direct annulation between a C–H bond on the aromatic core and a tethered alkyl moiety provides a straightforward approach to access these scaffolds; however, such a strategy is often hampered by the need of special reactive groups and/or less compatible cyclization conditions. It would be synthetically appealing if a common native functional group can be used as a handle to enable a general C–H annulation with diverse aromatic rings. Here, we show a deacylative annulation strategy for preparing a large variety of aromatic-fused rings from linear simple ketone precursors. The reaction starts with homolytic cleavage of the ketone α C–C bond via a pre-aromatic intermediate, followed by a radical-mediated dehydrogenative cyclization. Using widely available ketones as the robust radical precursors, this deconstructive approach allows streamlined assembly of complex polycyclic structures with broad functional group tolerance. [Figure not available: see fulltext.]

FUSED-RING OR TRICYCLIC ARYL PYRIMIDINE COMPOUND USED AS KINASE INHIBITOR

Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.

Pharmaceutical salt of novel EGRF (Epidermal Growth factor Receptor) kinase inhibitor as well as preparation method and application of pharmaceutical salt

The invention relates to pharmaceutical salt of a novel EGRF (Epidermal Growth factor Receptor) kinase inhibitor. Specifically, the invention relates to pharmaceutical salt of N-(2-(2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(6,7,8,9-tetrahydropyridine[1,2-a]indole-10-yl)-pyrimidine-2-yl)amino)phenyl) allyl-acylamide and preparation method; the pharmaceutical salt can be used for preparing a medicine which is used for treating and/or preventing tumors and has drug resistance.

Mesylate crystal of novel EGFR kinase inhibitor and preparation method

The invention relates to a mesylate crystal of a novel EGFR kinase inhibitor. Concretely, the invention relates to a mesylate crystal form of N-(2-((2-(dimethylamino)ethyl (methyl) amidogen)-4-methoxy-5-((4-(6,7,8,9-tetrahydropyridine[1,2-a]indol-10-base)-pyrimidine-2-base)amidogen)phenyl)acrylamide, and a preparation method. The crystal form can be used to preparing a medicine for treating and/orpreventing drug-resistant tumors.

New crystal forms of novel EGFR (epidermal growth factor receptor) kinase inhibitor and preparation method of new crystal forms

The invention relates to several new crystal forms of a novel EGFR (epidermal growth factor receptor) kinase inhibitor. Particularly, the invention relates to crystal forms of N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(6,7,8,9-tetrahydropyridino[1,2-a] indole-10-yl)-pyrimidin-2-yl)amino)phenyl)acrylamide and a preparation method. The crystal forms can be applied to preparation of drugs for treating and/or preventing drug-resistant tumors.

Visible-Light-Driven Palladium-Catalyzed Radical Alkylation of C?H Bonds with Unactivated Alkyl Bromides

Reported herein is a novel visible-light photoredox system with Pd(PPh3)4 as the sole catalyst for the realization of the first direct cross-coupling of C(sp3)?H bonds in N-aryl tetrahydroisoquinolines with unactivated alkyl bromides. Moreover, intra- and intermolecular alkylations of heteroarenes were also developed under mild reaction conditions. A variety of tertiary, secondary, and primary alkyl bromides undergo reaction to generate C(sp3)?C(sp3) and C(sp2)?C(sp3) bonds in moderate to excellent yields. These redox-neutral reactions feature broad substrate scope (>60 examples), good functional-group tolerance, and facile generation of quaternary centers. Mechanistic studies indicate that the simple palladium complex acts as the visible-light photocatalyst and radicals are involved in the process.

Palladium-Catalyzed, Ring-Forming Aromatic C-H Alkylations with Unactivated Alkyl Halides

A catalytic C-H alkylation using unactivated alkyl halides and a variety of arenes and heteroarenes is described. This ring-forming process is successful with a variety of unactivated primary and secondary alkyl halides, including those with β-hydrogens. In contrast to standard polar or radical cyclizations of aromatic systems, electronic activation of the substrate is not required. The mild, catalytic reaction conditions are highly functional group tolerant and facilitate access to a diverse range of synthetically and medicinally important carbocyclic and heterocyclic systems.