396074-50-3

Usage

Uses

Used in Pharmaceutical Industry:
(s)-tert-butyl 5-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide is used as a precursor for the synthesis of various drugs and functional molecules. Its unique structure and chemical properties make it a valuable intermediate in the development of new pharmaceutical compounds with potential therapeutic applications.
Used in Agrochemical Industry:
In the agrochemical industry, (s)-tert-butyl 5-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide is utilized as a building block for the synthesis of agrochemicals, such as pesticides and herbicides. Its diverse chemical properties and stability contribute to the development of effective and environmentally friendly agrochemical products.
Used in Organic Synthesis:
(s)-tert-butyl 5-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide is used as a versatile building block in organic synthesis. Its unique structure and reactivity make it a valuable intermediate for the synthesis of a wide range of organic compounds, including pharmaceuticals, agrochemicals, and other functional molecules.
Used in Medicinal Research:
The presence of the 1,2,3-oxathiazolidine-3-carboxylate moiety in (s)-tert-butyl 5-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide gives it potential pharmacological activity. It is used in medicinal research for further exploration of its therapeutic potential and the development of new drugs with novel mechanisms of action.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 167938-56-9 tert-butyl [(2S)-2-hydroxypropyl]carbamate 

Downstream Products

• 1338090-92-8 [(S)-2-(3-trifluoromethylphenyl)propyl]carbamic acid tert-butyl ester 

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.

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.

SOLID FORMS OF 3-((1R,3R)-1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)AZETIDIN-3-YL)AMINO)PHENYL)-3-METHYL-1,3,4,9-TETRAHYDRO-2H-PYRIDO[3,4-B]INDOL-2-YL)-2,2-DIFLUOROPROPAN-1-OL AND PROCESSES FOR PREPARING FUSED TRICYCLIC COMPOUNDS COMPRISING A SUBSTITUTED PHENYL OR PYRIDINYL MOIETY, INCLUDING METHODS OF THEIR USE

Provided herein are solid forms, salts such as compound B, and formulations of 3-((lR,3R)-l-(2,6-difluoro-4-((l-(3-fluoropropyl) azetidin-3-yl)amino)phenyl)-3-methyl-l,3,4,9-tetrahydro-2H- pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-l-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

HETEROCYCLIC COMPOUNDS CONTAINING A PYRROLOPYRIDINE OR BENZIMIDAZOLE CORE

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

HETEROCYCLIC COMPOUNDS CONTAINING AN INDOLE CORE

Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.

Ring opening of cyclic sulfamidates with bromophenyl metal reagents: Complementarity of sulfamidates and aziridines

Bromophenyl magnesium reagents generated via a Knochel type magnesium-halogen exchange of aryl iodides undergo regioselective ring opening of cyclic primary and secondary N-Boc sulfamidates in good to excellent yields. With secondary sulfamidates the reaction proceeds with clean inversion of the stereochemistry. This protocol complements the ring opening of aziridines with bromophenyl metal reagents and extends its scope to secondary substrates.

Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists

Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a- hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT2 receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT2C receptor agonists.

Anti-obesity 1,2,3,4,10,10-a-hexahydropy razino [1,2-a] indoles

The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a] indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

Piperazine derivatives

Piperazine derivatives, as well as pharmaceutically acceptable salts, solvates and esters thereof, can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central ner