31169-25-2

Usage

Uses

Used in Pharmaceutical Industry:
7-Bromothieno[3,2-d]pyrimidin-4(1H)-one is used as an intermediate reagent for the synthesis of various pharmaceutical compounds. Its unique structure and properties make it a key component in the development of new drugs and therapeutic agents.
Used in Organic Synthesis:
In the field of organic chemistry, 7-Bromothieno[3,2-d]pyrimidin-4(1H)-one serves as a versatile intermediate reagent. It is employed in the synthesis of a wide range of organic compounds, including complex molecules and potential drug candidates.

InChI:InChI=1/C6H3BrN2OS/c7-3-1-11-5-4(3)8-2-9-6(5)10/h1-2H,(H,8,9,10)

Upstream product

• 16234-10-9 3H-thieno[3,2-d]pyrimidin-4-one 
• 1383531-54-1 7-amino-3H-thieno[3,2-d]pyrimidin-4-one 
• 31169-26-3 7-nitro-3H-thieno[3,2-d]pyrimidin-4-one 
• 22288-78-4 Methyl 3-aminothiophene-2-carboxylate 
• 16285-69-1 3-(formylamino)-2-thiophenecarboxylic acid methyl ester 

Downstream Products

• 1318126-80-5 ethyl 3-((4-(2-hydroxyethylamino)thieno[3,2-d]pyrimidin-7-yl)ethynyl)-4-methyl benzoate 
• 1318132-90-9 ethyl 4-methyl-3-((4-(methylsulfinyl)thieno[3,2-d]pyrimidin-7-yl)ethynyl)benzoate 
• 1318132-88-5 ethyl 4-methyl-3-((4-(methylthio)thieno[3,2-d]pyrimidine-7-yl)ethynyl)benzoate 
• 1318128-91-4 4-amino-N-(3,5-dimethoxyphenyl)thieno[3,2-d]pyrimidine-7-carboxamide 
• 1318132-98-7 N-(3,5-dimethoxyphenyl)-4-(methylsulfinyl)thieno[3,2-d]pyrimidine-7-carboxamide 
• 1318132-97-6 N-(3,5-dimethoxyphenyl)-4-(methylthio)thieno[3,2-d]pyrimidine-7-carboxamide 
• 1269667-24-4 thieno[3,2-d]pyrimidine-7-carboxylic acid [2,6-dichloro-3-(propane-1-sulfonylamino)phenyl]amide 
• 1269666-83-2 4-cyclopropylaminothieno[3,2-d]pyrimidine-7-carboxylic acid [2,6-dichloro-3-(propane-1-sulfonylamino)phenyl]amide 
• 1269666-82-1 4-methoxyaminothieno[3,2-d]pyrimidine-7-carboxylic acid [2,6-dichloro-3-(propane-1-sulfonylamino)phenyl]amide 
• 1269667-70-0 N-(2-chloro-6-fluoro-3-(N-(4-methoxybenzyl)propylsulfonamido)phenyl)-4-methylthieno[3,2-d]pyrimidine-7-carboxamide 
• 1269666-26-3 4-aminothieno[3,2-d]pyrimidine-7-carboxylic acid [6-chloro-2-fluoro-3-(3-fluoro-propane-1-sulfonylamino)phenyl]amide 
• 1269667-61-9 4-chloro-N-(6-chloro-2-fluoro-3-(3-fluoropropylsulfonamido)phenyl)thieno[3,2-d]pyrimidine-7-carboxamide 
• 1269666-24-1 4-aminothieno[3,2-d]pyrimidine-7-carboxylic acid (3-benzenesulfonylamino-2,6-difluoro-phenyl)amide 
• 1269666-22-9 4-aminothieno[3,2-d]pyrimidine-7-carboxylic acid [2,6-dichloro-3-(propane-1-sulfonylamino)phenyl]amide 

Relevant academic research and scientific papers

An Efficient Second-Generation Manufacturing Process for the pan-RAF Inhibitor Belvarafenib

Herein, the development of a streamlined manufacturing process for the pan-RAF inhibitor belvarafenib (GDC-5573) is reported. The process to belvarafenib features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access the penultimate intermediate 3. The final amide coupling was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate as the coupling reagent, which afforded belvarafenib on a multikilogram production scale after recrystallization.

FUSED PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON FMS KINASES

Disclosed are a fused pyrimidine derivative of formula (I), and a pharmaceutically acceptable salt, stereoisomer, hydrate and solvate thereof, which have an excellent inhibitory activity on FMS kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating diseases caused by abnormal activation of FMS kinases such as immunologic diseases, metabolic diseases, inflammatory diseases, cancers and tumors.

THIENO[3,2-D]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES

Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.

NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION INCLUDING SAME AS AN ACTIVE INGREDIENT

The present invention relates to a compound represented by formula (I) for inhibiting the activity of diacylglycerol O-acyltransferase type 1 (DGAT1), and pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising same as an active ingredient. The compound of the present invention may be used effectively in the treatment or prevention of a disease or condition mediated by the activity of DGAT1 such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, and the like, without any adverse effects: wherein A, B, X, and R5 to R7 are the same as defined in the specification.

NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION INCLUDING SAME AS AN ACTIVE INGREDIENT

The present invention relates to a compound represented by formula (I) for inhibiting the activity of diacylglycerol O-acyltransferase type 1 (DGAT1), and pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising same as an active ingredient. The compound of the present invention may be used effectively in the treatment or prevention of a disease or condition mediated by the activity of DGAT1 such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, and the like, without any adverse effects: wherein A, B, X, and R5 to R7 are the same as defined in the specification.

THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES

The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.

THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES

Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases

NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS

The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties

Recent clinical data provided proof-of-concept for selective B-Raf inhibitors in treatment of B-RafV600E mutant melanoma. Pyrazolopyridine-type B-Raf inhibitors previously described by the authors are potent and selective but exhibit low solubility requiring the use of amorphous dispersion-based formulation for achieving efficacious drug exposures. Through structure-based design, we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved solubility and pharmacokinetic profiles. The hinge binding moiety possesses a basic center imparting high solubility at gastric pH, addressing the dissolution limitation observed with our previous series. In our search for an optimal linker-hinge binding moiety system, amide-linked thieno[3,2-d]pyrimidine analogues 32 and 35 (G945), molecules with desirable physicochemical properties, emerged as lead compounds with strong efficacy in a B-RafV600E mutant mouse xenograft model. Synthesis, SAR, lead selection, and evaluation of key compounds in animal studies will be described.

Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening

Ligand efficient fragments binding to PDK1 were identified by an NMR fragment-based screening approach. Computational modeling of the fragments bound to the active site led to the design and synthesis of a series of novel 6,7-disubstituted thienopyrimidin