165107-97-1

Upstream product

• 108-24-7 acetic anhydride 
• 80517-22-2 2-amino-4-fluorobenzonitrile 
• 351-28-0 N-(3-fluorophenyl)acetamide 

Downstream Products

• 936363-99-4 C₁₁H₁₃FN₂O₂ 
• 162012-67-1 N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine 
• 936558-11-1 7-(2-aminoethoxy)-N-(3-chloro-4-fluorophenyl)-6-nitro-4-quinazolinamine 
• 936558-10-0 2-(4-(3-chloro-4-fluorophenylamino)-6-nitro-quinazolin-7-oxy)ethyl tert-butylcarbamate 
• 870562-74-6 2-(aminomethyl)-5-fluorobenzenamine hydrochloride 

Relevant academic research and scientific papers

Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities – Part 1

Overexpression of EGFR and HER2 are observed in many breast, ovarian, colon and prostate cancers. The second and third generation irreversible EGFR/HER2 dual kinase inhibitors became popular after the approval of Afatinib by FDA to overcome the mutation related problem. To find efficacious drug candidates, a series of novel quinazoline derivatives were designed, synthesized and evaluated as dual EGFR/HER2 tyrosine kinase (TK) inhibitors. Selected twenty four compounds were reported here with significant inhibitory activities against EGFR/HER2 tyrosine kinases. Several compounds showed nanomolar IC50 values. In vitro studies of quinazoline derivatives were done on NCI-H1975, HCC827, A431, MDA MB-453 cell lines. The compounds 1a, 1d and 1v were found more potent compared to standard drug afatinib. In vivo efficacy study of 1d on nude mice NCI-H1975 tumour xenograft model was discussed.

QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF

Disclosed are a quinazoline derivative, a preparation method therefor, and a pharmaceutical composition and an application thereof. The present invention provides a compound represented by general formula I, a stereoisomer thereof and a pharmaceutical acceptable salt or a solvate thereof. The quinazoline derivative of the present invention has a unique chemical structure, is characterized by irreversibly inhibiting EGFR tyrosine kinase, has high biological activity, apparently improves the inhibiting effect on the EGFR tyrosine kinase, has quite strong tumor inhibiting effect on tumor cells and a transplantation tumor pathological model of animal tumors, and has good market developing prospects.

Palladium-Catalyzed Regioselective Direct Cyanation of Acetanilide Derivatives with K4[Fe(CN)6] by C–H Bond Activation

A practical, versatile, and efficient method for the palladium-catalyzed direct cyanation of readily available acetanilides with K4[Fe(CN)6] as a safe cyanating agent through C–H bond activation with excellent C2 regioselectivity was developed. This finding represents a new strategy for the synthesis of N-(2-cyanoaryl)acetamides, which are important structural motifs in natural products and pharmaceuticals.

HIV integrase inhibitors

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

HIV INTEGRASE INHIBITORS

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS

The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Bicyclic heterocycles as HIV integrase inhibitors

The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.