209959-33-1

Usage

Uses

Used in Pharmaceutical Synthesis:
2-[BIS(TERT-BUTOXYCARBONYL)AMINO]-5-BROMOPYRIMIDINE is used as an intermediate in the synthesis of pharmaceuticals and other organic compounds. Its unique structure and protective t-Boc groups make it a valuable building block for the development of new drugs and organic molecules.
Used in Organic Synthesis:
In the field of organic synthesis, 2-[BIS(TERT-BUTOXYCARBONYL)AMINO]-5-BROMOPYRIMIDINE is used as a key intermediate for the preparation of various organic compounds. Its pyrimidine core and bromine atom at the 5th position provide opportunities for further functionalization and modification, enabling the synthesis of a wide range of organic molecules with diverse applications.
Used in Research and Development:
2-[BIS(TERT-BUTOXYCARBONYL)AMINO]-5-BROMOPYRIMIDINE is also utilized in research and development settings, where it can be employed to study the properties and reactivity of pyrimidine derivatives. Its unique structure and protective t-Boc groups make it an interesting subject for exploration in academic and industrial research labs.

InChI:InChI=1/C14H20BrN3O4/c1-13(2,3)21-11(19)18(12(20)22-14(4,5)6)10-16-7-9(15)8-17-10/h7-8H,1-6H3

Upstream product

• 7752-82-1 5-bromo-2-aminopyrimidine 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 883231-23-0 tert-butyl (5-bromopyrimidin-2-yl)carbamate 
• 914377-34-7 2-(5-hydroxy-2-pyrimidinyl)imidodicarbonic acid 1,3-bis(1,1-dimethylethyl)ester 

Relevant academic research and scientific papers

4-ETHYLNYLPYRIDINE DERIVATIVES USEFUL AS GCN2 INHIBITORS

The invention relates to compounds of formula I, wherein the substituents are as defined in more detail in the description. The compounds are potent inhibitors of GCN2 and have excellent pharmacokinetic properties. Compounds are useful for the treatment or prevention of various conditions, especially cancer. The invention further relates to pharmaceutical compositions comprising the compounds of the invention and uses of the compounds and compositions.

Compounds for treating spinal muscular atrophy

Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.

cGAS ANTAGONIST COMPOUNDS

Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer’s Agents Based on Rational Design

Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of β-amyloid peptides (pGlu-Aβ) and thus may participate in the pathogenesis of Alzheimer’s disease (AD). We designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, Aβ3E?42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions. This potent Aβ-lowering effect was achieved by incorporating an additional binding region into our previously established pharmacophoric model, resulting in strong interactions with the carboxylate group of Glu327 in the QC binding site. Our study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.

COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY

Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.

1,4-BENZODIAZEPINONE COMPOUNDS AND THEIR USE IN TREATING CANCER

The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided.

NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE

The present invention relates to pyrimidinones and pyridones and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

Nitrogen containing heteroaromatics as factor Xa inhibitors

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP

The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.