459817-82-4

Usage

Uses

Used in Organic Synthesis:
Tert-Butyl 1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide is used as a protective group for carbonyl compounds in organic synthesis for its high selectivity in forming reversible complexes with these groups, thereby safeguarding them from unwanted reactions.
Used in Scientific Research:
In the realm of scientific research, Tert-Butyl 1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide is employed to study and develop new organic synthesis methods, given its unique protective properties for carbonyl compounds.
Used in Industrial Applications:
Although its broader industrial applications are not explicitly detailed, Tert-Butyl 1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide's role in organic synthesis suggests potential use in the development of new chemical compounds and materials within various industries that rely on advanced organic chemistry.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 26690-80-2 2-(N-tert-butoxycarbonylamino)ethanol 

Downstream Products

• 19044-42-9 [1,2,3]-oxathiazolidine-2,2-dioxide 
• 521266-41-1 (2S)-1-{[2-(3-N,N-dimethylamino-phenoxy)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile 
• 1613623-72-5 {2-[5-(3-chlorophenyl)-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrrolo[3,4-d]pyrimidin-6-yl]ethyl}carbamic acid tert-butyl ester 
• 178181-52-7 tert-butyl (2-fluoroethyl)carbamate 
• 1056015-76-9 tert-butyl [2-(2-iodophenoxy)ethyl]carbamate 
• 887590-25-2 3,4-dihydro-2H-quinoxaline-1-carboxylic acid tert-butyl ester 
• 1441005-75-9 C₁₃H₁₉BrN₂O₂ 
• 1204333-53-8 C₁₃H₁₈BrNO₃ 
• 1453206-80-8 (3R,4S)-tert-butyl 3-(2-((tert-butoxycarbonyl)amino)ethyl)-2,5-dioxo-1,4-diphenylpyrrolidine-3-carboxylate 

Relevant academic research and scientific papers

Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation

As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key drug target in solid tumors. However, the use of the First-generation Trk inhibitors was greatly restricted due to mutant drug resistance. Fortunately, the emergence of the Second-generation of Trk inhibitors has brought an effective solution to this mutant resistance, such as TPX-0005 (Repotrectinib). Here, we reported a series of pyrizolo[1,5-a]pyrimidine derivatives as the second-generation Trk inhibitors, and carried out the subsequent biological activity evaluation. Among them, the best compound 14h (IC50 = 1.40, 1.80 nM, against TrkA, TrkAG595R, respectively) and 14j (IC50 = 0.86, 6.92 nM, against TrkA, TrkAG595R, respectively) has a kinase activity comparable to TPX-0005, and 14j (IC50 = 350 nM against ALK) has a higher selectivity of Trk inhibition than TPX-0005, which may be of great significance for reducing toxicity.

Method for preparing 2-methoxyethylamine hydrochloride

The invention relates to a method for preparing 2-methoxyethylamine. The method comprises the following steps: carrying out ring closing reaction on N-Boc-ethanolamine serving as an original materialto generate 1, 2, 3-oxathiazolidine tert-butyl-3-carboxylate-2-oxide, oxidizing to obtain 1, 2, 3-oxathiazolidine tert-butyl-3-carboxylate-2, 2-dioxide, and carrying out ring opening reaction with methanol to obtain N-Boc-2-methoxyethylamine, and removing the Boc protecting group to obtain the 2-methoxyethylamine hydrochloride. According to the method, the use of a high-toxicity methylation reagent is avoided, meanwhile, the generation of N-methylation impurities is completely avoided, the quality control of raw material medicines is facilitated, and the method is environmentally friendly, mild in reaction condition, simple and convenient to operate and suitable for industrial production.

Substituted chiral diaryl macrocyclic compound as TRK inhibitors

The invention relates to a substituted chiral diaryl macrocyclic compound as a TRK inhibitor, and belongs to the technical field. The structure of the chiral diaryl macrocyclic compound is shown as a general formula (I), and the chiral diaryl macrocyclic

Synthesis method for tert-butyl 1,2,3-oxathiazolidine-3-carboxylic ester 2,2-dioxide compound

The invention relates to a synthesis method for a tert-butyl 1,2,3-oxathiazolidine-3-carboxylic ester 2,2-dioxide compound. The tert-butyl 1,2,3-oxathiazolidine-3-carboxylic ester 2,2-dioxide compoundhas a structural formula as shown in a formula I which is described in the specification. The synthesis method comprises the step of allowing a compound as shown in a formula II which is described inthe specification with sulfonyl chloride in the presence of an organic solvent to generate the compound as shown in the formula I. The structural formula of the compound as shown in the formula I andthe structural formula of the compound as shown in the formula II are described in the specification. The synthesis method disclosed by the invention is simple to operate; compared with a conventional published two-step method, the synthesis method provided by the invention only needs one step; and the synthesis method is more convenient, reduces byproducts, is high in yield, does not need to usea catalyst and a highly-toxic substance in the reaction, and is safe and low in cost.

Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase

Historically, chemists have explored chemical space in a highly uneven and unsystematic manner. As an example, the shape diversity of existing fragment sets does not generally reflect that of all theoretically possible fragments. To assess experimentally the added value of increased three dimensionality, a shape-diverse fragment set was designed and collated. The set was assembled by both using commercially available fragments and harnessing unified synthetic approaches to sp3-rich molecular scaffolds. The resulting set of 80 fragments was highly three-dimensional, and its shape diversity was significantly enriched by twenty synthesised fragments. The fragment set was screened by high-throughput protein crystallography against Aurora-A kinase, revealing four hits that targeted the binding site of allosteric regulators. In the longer term, it is envisaged that the fragment set could be screened against a range of functionally diverse proteins, allowing the added value of more shape-diverse screening collections to be more fully assessed.

A kind of IDO inhibitor and use thereof

The embodiment of the invention provides general formula (I) compound or its pharmaceutically acceptable salts, stereoisomers, a tautomeric form each other, polymorphs, solvate, prodrug, metabolite or isotope derivatives, wherein the substituents R1

Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC)

The RAS/MAPK pathway is a major driver of oncogenesis and is dysregulated in approximately 30% of human cancers, primarily by mutations in the BRAF or RAS genes. The extracellular-signal-regulated kinases (ERK1 and ERK2) serve as central nodes within this pathway. The feasibility of targeting the RAS/MAPK pathway has been demonstrated by the clinical responses observed through the use of BRAF and MEK inhibitors in BRAF V600E/K metastatic melanoma; however, resistance frequently develops. Importantly, ERK1/2 inhibition may have clinical utility in overcoming acquired resistance to RAF and MEK inhibitors, where RAS/MAPK pathway reactivation has occurred, such as relapsed BRAF V600E/K melanoma. We describe our structure-based design approach leading to the discovery of AZD0364, a potent and selective inhibitor of ERK1 and ERK2. AZD0364 exhibits high cellular potency (IC50 = 6 nM) as well as excellent physicochemical and absorption, distribution, metabolism, and excretion (ADME) properties and has demonstrated encouraging antitumor activity in preclinical models.

BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY

The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- mac

Nucleophilic Trifluoromethylthiolation of Cyclic Sulfamidates: Access to Chiral β- And γ-SCF3 Amines and α-Amino Esters

The regio- and stereoselective ring opening of 1,2- and 1,3-sulfamidates with trifluoromethanethiolate anion is reported. This direct introduction of the whole SCF3 motif is a straightforward synthetic route toward β- and γ-SCF3 amines and α-amino acid derivatives. The utility of this reaction was further illustrated by incorporation of Cys(S-CF3) into di- and tripeptides.

Copper-catalysed cross-coupling affected by the Smiles rearrangement: A new chapter on diversifying the synthesis of chiral fluorinated 1,4-benzoxazine derivatives

Synthesis of different chiral fluorinated Boc-[1,4]benzoxazins from their open chain precursors were investigated. The NMR spectra and crystallographic data showed the presence of the Smiles Rearrangement (SR) followed by copper catalysed coupling. The in