42839-09-8

Usage

Uses

Used in Pharmaceutical Industry:
2-Pyrimidinemethanol is used as a reactant for the synthesis of avanafil, a medication used to treat erectile dysfunction. It plays a crucial role in the development of this drug, contributing to its effectiveness in addressing the sexual health concerns of patients.
Additionally, 2-Pyrimidinemethanol is utilized in the synthesis of other pharmaceutical compounds, showcasing its versatility and importance in the development of novel medications for various health conditions. Its chemical structure allows for further modification and functionalization, making it a valuable building block in the creation of new drugs with potential therapeutic benefits.

InChI:InChI=1/C5H6N2O/c8-4-5-6-2-1-3-7-5/h1-3,8H,4H2

Upstream product

• 22433-12-1 (5-bromopyrimidine-2-yl)methanol 
• 34253-03-7 pyrimidine-2-carboxylic acid methyl ester 
• 14080-23-0 2-cyanopyrimidine 
• 31519-62-7 pyrimidine-2-carboxylic acid 

Downstream Products

• 324572-92-1 2-((2-methylpyridin-4-yl)methyl)-4-(3,4,5-trimethoxyphenyl)-8-((pyrimidin-2-yl)methoxy)-1,2-dihydro-1-oxo-2,7-naphthyridine-3-carboxylic acid methyl ester 
• 1261171-61-2 C₁₇H₁₈Cl₂N₄O₂ 
• 1330115-12-2 (9H-Fluoren-9-yl)methyl (4-benzamido-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl(1,3-dihydroxypropan-2-yl)carbamate 
• 1351764-50-5 (S)-N-(5-(2,4-dichloro-6-ethoxyphenyl)-1-(4-methoxybenzyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-5-fluoro-2-(pyrimidin-2-ylmethoxy)nicotinamide 
• 1351764-04-9 N-(5-(2,4-dichloro-6-ethoxyphenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-5-fluoro-2-(pyrimidin-2-ylmethoxy)nicotinamide 
• 1351764-49-2 (S)-N-(5-(2,4-dichloro-6-ethoxyphenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-5-fluoro-2-(pyrimidin-2-ylmethoxy)nicotinamide 
• 1351764-51-6 (R)-N-(5-(2,4-dichloro-6-ethoxyphenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-5-fluoro-2-(pyrimidin-2-ylmethoxy)nicotinamide 
• 1585206-25-2 2-({2-[2-(3-methoxyphenyl)ethyl]phenoxy}methyl)pyrimidine 
• 59566-45-9 2-(pyrimidin-2-yl)acetonitrile 
• 60561-50-4 methyl 2-(pyrimidin-2-yl)acetate 
• 27427-92-5 pyrimidine-2-carbaldehyde 

Relevant academic research and scientific papers

Asymmetric zinc porphyrin derivatives bearing three pseudo-pyrimidine: Meso -position substituents and their photosensitization for H2evolution

Novel asymmetric zinc porphyrin derivatives (ZnPy-5 and ZnPy-6) with meso-positions bearing one benzoic acid and three pseudo-pyrimidines with two N atoms located at different positions were synthesized and utilized as sensitizers for Pt-loaded g-C3N4 (PCN). Compared to the analogue (ZnPy-1 bearing one benzoic acid and three phenyl meso-position substituents), ZnPy-5 and ZnPy-6 exhibit significantly enhanced photosensitization on PCN under visible light (λ ≥ 420 nm) illumination. In particular, ZnPy-5/PCN and ZnPy-6/PCN exhibit H2 evolution activities of 418 and 585 μmol h-1, corresponding to turnover numbers (TON) of 8845 and 12?381 h-1, respectively. Both of these values are much better that (316 μmol h-1) of ZnPy-1/PCN, which has a TON of 6687 h-1. In addition, ZnPy-5/PCN and ZnPy-6/PCN show apparent quantum yields of 32.6% and 33.1% at 420 nm monochromatic light, and these are much higher than that (10.6%) for ZnPy-1/PCN. Compared with ZnPy-5, the two N atoms of the pseudo-pyrimidines in ZnPy-6 are further away from the porphyrin macrocycle, which can more effectively combine with the sacrificial reagent and g-C3N4, thus promoting dye regeneration and the photoexcited charge transfer for delivering better photocatalytic performance. The present results demonstrate that the number and positions of the N atoms in the peripheral substituents of the porphyrin derivatives have a great influence on the photosensitization, and that the fine-tuning of molecular structures is crucial for improving the H2 evolution activity of the dye-sensitized semiconductors.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity

Cruzain, an essential cysteine protease of the parasitic protozoan, Trypanosoma cruzi, is an important drug target for Chagas disease. We describe here a new series of reversible but time-dependent inhibitors of cruzain, composed of a dipeptide scaffold appended to vinyl heterocycles meant to provide replacements for the irreversible reactive "warheads" of vinyl sulfone inactivators of cruzain. Peptidomimetic vinyl heterocyclic inhibitors (PVHIs) containing Cbz-Phe-Phe/homoPhe scaffolds with vinyl-2-pyrimidine, vinyl-2-pyridine, and vinyl-2-(N-methyl)-pyridine groups conferred reversible, time-dependent inhibition of cruzain (Ki? = 0.1-0.4 μM). These cruzain inhibitors exhibited moderate to excellent selectivity versus human cathepsins B, L, and S and showed no apparent toxicity to human cells but were effective in cell cultures of Trypanosoma brucei brucei (EC50 = 1-15 μM) and eliminated T. cruzi in infected murine cardiomyoblasts (EC50 = 5-8 μM). PVHIs represent a new class of cruzain inhibitors that could progress to viable candidate compounds to treat Chagas disease and human sleeping sickness.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol "APLNR"). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

COMPOUNDS AND RELATED COMPOSITIONS AND METHODS OF USE

Compounds and compositions, which can be use for example, for treating cancer, are described herein.

IMIDAZOTRIAZINONE COMPOUNDS

The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9 and pharmaceutically acceptable salt thereof. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.

IMIDAZOTRIAZINONE COMPOUNDS

The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including CNS or neurodegeneration disorder.

Saporin-L1 inhibitors and uses thereof

Inhibitors of saporin-L1 are disclosed, as are related compositions and uses thereof, in particular in cancer therapy that employs saporin-L1-linked immunotoxins.

RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF

Compounds of Formulas (I), (IIA) and (IIIA) are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formulas (I), (IIA) and (IIIA) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Raf inhibitor compounds and methods of use thereof

Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.