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Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1

Bone Morphogenetic Protein 1 (BMP1) inhibition is a potential method for treating fibrosis because BMP1, a member of the zinc metalloprotease family, is required to convert pro-collagen to collagen. A novel class of reverse hydroxamate BMP1 inhibitors was discovered, and cocrystal structures with BMP1 were obtained. The observed binding mode is unique in that the small molecule occupies the nonprime side of the metalloprotease pocket providing an opportunity to build in metalloprotease selectivity. Structure-guided modification of the initial hit led to the identification of an oral in vivo tool compound with selectivity over other metalloproteases. Due to irreversible inhibition of cytochrome P450 3A4 for this chemical class, the risk of potential drug-drug interactions was managed by optimizing the series for subcutaneous injection.

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Reference:
Oxazolidine – Wikipedia,
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Directed orthometalation and the asymmetric total synthesis of N -deoxymilitarinone A and torrubiellone B

A diverted total synthesis (DTS) approach to the total synthesis of pyridone alkaloids N-deoxymilitarinone A (8) and torrubiellone B (10) has been developed. The common intermediate 14 was first assembled by a dual directed orthometalation process using a methoxymethyl group as directed metalation group. Other crucial steps include the assembly of polyenes under aldol condensation for DTS using general and concise strategy and diastereoselective synthesis of the syn-dimethyl array by an Evans aldol reaction.

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Oxazolidine – Wikipedia,
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SONIC HEDGEHOG MODULATORS

The present invention relates to relates to macrocyclic small molecule inhibitors of the Sonic Hedgehog signaling pathway, syntheses thereof, and intermediates thereto. Such small molecule modulators of the Sonic Hedgehog signaling pathway are useful in the treatment of proliferative diseases (e.g., basal cell carcinoma, Gorlin syndrome, medulloblastoma, or pancreatic cancer), pulmonary diseases (e.g., interstitial pnuemonitis or interstitial pulmonary fibrosis), and developmental disorders (e.g., phocomelia or cyclopia). Novel non-natural macrocycles are provided that inhibit Sonic Hedgehog induced-protein transcription.

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Reference:
Oxazolidine – Wikipedia,
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Acyl transfer catalysis with 1,2,4-Triazole anion

1,2,4-Triazole anion has been identified as an active acyl transfer catalyst suitable for the aminolysis and transesterification of esters.

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COMBINATIONS OF AKT INHIBITOR COMPOUNDS AND VEMURAFENIB, AND METHODS OF USE

The invention provides a combination of a) a compound of Formula 1a: [insert Formula 1a], or a pharmaceutically acceptable salt there- of, and b) vemurafenib or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of a hyperproliferative disorder, such as cancer.

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Oxazolidine – Wikipedia,
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Asymmetric synthesis of dideazafolate antitumor agents via amidomethylation of nonracemic oxazolidinone imidates, synthesis of LY309887, a cytotoxic dideazafolate analog related to lometrexol

The asymmetric synthesis of LY309887, a cytotoxic dideazatetrahydrofolate analog related to lometrexol, has been accomplished via an application of diastereoselective amidomethylation of a chiral titanium (IV) acyloxazolidinone enolate.

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Oxazolidine – Wikipedia,
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New explortion of (R)-4-Benzyl-2-oxazolidinone

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Related Products of 102029-44-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 102029-44-7, molcular formula is C10H11NO2, introducing its new discovery.

5-AMINO-4-CARBAMOYL-PYRAZOLE COMPOUNDS AS SELECTIVE AND IRREVERSIBLE T790M OVER WT-EGFR KINASE INHIBITORS AND USE THEREOF????

Disclosed are compounds of Formula (I), pharmaceutical compositions comprising the same, processes for the preparation thereof, and the use thereof.

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Oxazolidine – Wikipedia,
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An efficient asymmetric synthesis of furofuran lignans: (+)-Sesamin and (-)-sesamin

An efficient synthesis of (+)-sesamin 1a and (-)-sesamin 1b is described. The key reactions include highly stereoselective aldol condensation of piperonal 7 with the dianion of chiral oxazolidinone 8, followed by intramolecular ring cyclization of aldol product 11 in high yield.

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Total synthesis of (+)-A83543A [(+)-lepicidin A]

The first synthesis of the macrolide insecticide A83543A (lepicidin A) has been completed using a Diels-Alder strategy to construct the carbocyclic framework. Diene synthesis through Pd-catalyzed Stille coupling of a macrocyclic vinylstannane and suitably functionalized vinyl iodide was followed by a diastereoselective Lewis acid-mediated intramolecular Diels-Alder reaction to construct the trans hydrindene subunit. Refunctionalization and intramolecular aldol condensation afforded the differentially protected (+)-lepicidin A aglycon. Successive glycosidations with 2,3,4-tri-O-methyl-D-rhamnose and N-protected L-forosamine followed by deprotection and methylation completed the synthesis of the enantiomer of the natural product.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1813NO – PubChem

 

Extracurricular laboratory:new discovery of 102029-44-7

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 102029-44-7

Synthetic Route of 102029-44-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.102029-44-7, Name is (R)-4-Benzyl-2-oxazolidinone, molecular formula is C10H11NO2. In a Article,once mentioned of 102029-44-7

Synthetic studies toward (+)-spongidepsin

A convergent enantiomerically controlled synthetic effort toward (+)-spongidepsin is reported. The synthesis benefits from the use of readily available and inexpensive starting materials like D-mannitol and (-)-beta-citronellene. Key transformations include Evans asymmetric methylation, Mitsunobu esterification, (1H-benzotriazol-1-yloxy) tripyrrolidinophosphonium hexafluorophosphate (PyBOP)-mediated amide formation for the preparation of a fully functionalized acyclic precursor, and ring-closing metathesis (RCM). Copyright

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H2063NO – PubChem