281234-03-5

Upstream product

• 530-62-1 1,1'-carbonyldiimidazole 
• 184778-33-4 4-(N-hydroxycarbamimidoyl)-benzoic acid methyl ester 
• 1076-96-6 methyl 4-vinylbenzoate 
• 65695-05-8 methyl 4-(N’-hydroxycarbamimidoyl)benzoate 
• 1129-35-7 4-cyanobenzoic acid methyl ester 
• 184778-33-4 methyl (Z)-4-(N’-hydroxycarbamimidoyl)benzoate 

Downstream Products

• 1370330-82-7 methyl 4-(4,5-dihydro-5-oxo-4-(3-(5-oxo-3-phenyl-1,2,4-oxadiazol-4-yl)propyl)-1,2,4-oxadiazol-3-yl)benzoate 
• 1370330-83-8 C₁₈H₂₀N₄O₄ 
• 340736-41-6 methyl 2-[(2S)-4-[2-(tert-butoxy)-2-oxoethyl]-1-[(2S)-3-(4-methoxyphenyl)-2-[[4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoyl]-3-oxopiperazinyl]acetate 
• 189365-92-2 4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)benzoic acid 

Relevant academic research and scientific papers

Cobalt-Catalyzed, Directed Intermolecular C-H Bond Functionalization for Multiheteroatom Heterocycle Synthesis: The Case of Benzotriazine

Transition-metal-catalyzed, directed intermolecular C-H bond functionalization is synthetically useful but heavily underexplored in multiheteroatom heterocycle synthesis. Herein we report a cobalt catalytic method for the formation of a three-nitrogen-bearing benzotriazine scaffold via the coupling of arylhydrazine and oxadiazolone. This synthetic protocol features a low-cost base metal catalyst, a maximum number of heteroatoms built into a heterocycle, a distinct synthetic logic for benzotriazines, a superior step economy, and a broad substrate scope.

Tert-Butyl Nitrite Mediated Synthesis of 1,2,4-Oxadiazol-5(4 H)-ones from Terminal Aryl Alkenes

tert-Butyl nitrite (TBN) mediated synthesis of 3-aryl-1,2,4-oxadiazol-5(4H)-ones has been accomplished using terminal aryl alkenes via a biradical reaction intermediate. Three consecutive sp2 C-H bond functionalizations of styrenes afforded 3-phenyl-1,2,4-oxadiazol-5(4H)-ones via the formation of new C?N, C?O, C-O, and two C-N bonds. Both of the N atoms originate from TBN, while the carbonyl oxygen is from the water (moisture) the other oxygen from the N?O part of the TBN.

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

A novel bifunctional chelating agent based on bis(hydroxamamide) for 99mTc labeling of polypeptides

This paper describes the synthesis and biological evaluation of a novel bifunctional chelating agent (BCA) based on bis(hydroxamamide) for 99mTc labeling of polypeptides. We successfully designed and synthesized C3(BHam)2·COOH as a new BCA. C 3(BHam)2·COOH formed a stable 99mTc complex and enabled us to prepare 99mTc-labeled polypeptides by using a 2,3,5,6-tetrafluorophenol (TFP) active ester of C3(BHam) 2·COOH. 99mTc-C3(BHam) 2·HSA prepared with C3(BHam)2·TFP was stable in both murine plasma and an excess of l-cysteine without any dissociation of 99mTc from polypeptides. Furthermore, the blood clearance of 99mTc-C3(BHam)2·HSA in mice was similar to that of 125I-HSA, suggesting that C 3(BHam)2·COOH retained stable binding between 99mTc and the polypeptides in vivo. When 99mTc-C 3(BHam)2·NGA was injected into mice, the radioactivity showed high hepatic uptake early on and a rapid clearance from the liver, indicating that C3(BHam)2·COOH did not affect the pharmacokinetics of polypeptides in vivo and gave radiometabolites, which displayed a rapid elimination from the liver. Such characteristics would render C3(BHam)2·COOH attractive as a new BCA for 99mTc labeling of polypeptides. Copyright

MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF

The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.

Orally active GPIIb/IIIa antagonists: Synthesis and biological activities of masked amidines as prodrugs of 2-[(3S)-4-[(2S)-2-(4-amidinobenzoylamino)-3-(4-methoxyphenyl)propanoyl]-3- (2-methoxy-2-oxoethyl)-2-oxopiperazinyl]acetic acid

To improve the in vivo potency of the potent GPIIb/IIIa antagonist 2-[(3S)-4-[(2S)-2-(4-amidinobenzoylamino)-3-(4-methoxyphenyl)propanoyl]-3- (2-methoxy-2-oxoethyl)-2-oxopiperazinyl]lacetic acid (4), the amidino group was converted to an oxadiazole ring, thiadiazole ring of substituted amidoxime group. These groups were expected to be metabolized to an amidino group in vivo. The compounds synthesized were evaluated for their potency to inhibit the ex vivo adenosine 5′-diphosphate (ADP)-induced aggregation of guinea pig platelets. Among the compounds examined, the methoxycarbonyloxyamidine 8a exhibited the most potent ex vivo inhibitory activity with a fast onset and prolonged duration of action after oral administration.