439948-91-1

Usage

Uses

Used in Pharmaceutical Industry:
Tert-butyl(4S)-4-methyl-2,2-dioxo-1,2λ,3-oxathiazolidine-3-carboxylate is used as a reagent in the production of various pharmaceuticals. Its unique structure and reactivity enable the synthesis of complex organic compounds with potential therapeutic applications.
Used in Organic Synthesis:
In the field of organic synthesis, tert-butyl(4S)-4-methyl-2,2-dioxo-1,2λ,3-oxathiazolidine-3-carboxylate serves as a building block for the synthesis of more complex chemical compounds. The tert-butyl group provides stability and protection to the reactive parts of the molecule, facilitating a variety of chemical reactions.
Used as a Protecting Group:
The tert-butyl group in tert-butyl(4S)-4-methyl-2,2-dioxo-1,2λ,3-oxathiazolidine-3-carboxylate can be used as a protecting group in organic synthesis. It shields reactive functional groups from unwanted side reactions, allowing for selective reactions to occur at other sites within the molecule.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 79069-13-9 (S)-2-t-butoxycarbonylaminopropan-1-ol 
• 950852-76-3 tert-butyl (4S)-4-methyl-2-oxido-1,2,3-oxathiazolidin-2-ium-3-carboxylate 

Downstream Products

• 521266-43-3 (S)-[2-(4-N,N-Dimethylamino-phenyl)-1-methyl-ethyl]-carbamic Acid Tert-Butyl Ester 
• 913979-61-0 C₂₀H₂₈FN₃O₃ 
• 941596-56-1 5-benzyloxy-1-((S)-2-tert-butoxycarbonylamino-propyl)-1H-indole-2-carboxylic acid ethyl ester 
• 204926-09-0 C₁₄H₂₀BrNO₃ 
• 1441005-57-7 C₁₅H₂₂BrNO₃ 
• 1441005-54-4 C₁₄H₂₀INO₃ 
• 1185454-25-4 C₁₄H₁₈BrF₂NO₃ 
• 74192-91-9 (S)-1-(diphenylphosphino)-2-propanamine 
• 1338090-91-7 [(S)-1-methyl-2-(3-trifluoromethylphenyl)ethyl]carbamic acid tert-butyl ester 
• 1338090-97-3 [(S)-2-(4-bromophenyl)-1-methylethyl]carbamic acid tert-butyl ester 
• 1338090-95-1 [(S)-2-(3-bromophenyl)-1-methylethyl]carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Cobalt-Catalyzed Desymmetric Isomerization of Exocyclic Olefins

Chiral cyclic olefins, 1-methylcyclohexenes, are versatile building blocks for the synthesis of pharmaceuticals and natural products. Despite the prevalence of these structural motifs, the development of efficient synthetic methods remains an unmet challenge. Herein we report a novel desymmetric isomerization of exocyclic olefins using a series of newly designed chiral cobalt catalysts, which enables a straightforward construction of chiral 1-methylcyclohexenes with diversified functionalities. The synthetic utility of this methodology is highlighted by a concise and enantioselective synthesis of a natural product, β-bisabolene. The versatility of the reaction products is further demonstrated by multifarious derivatizations.

COMPOUNDS FOR TREATING FAMILIAL DYSAUTONOMIA

The present description relates to compounds useful for improving pre-mRNA splicing in a cell. In particular, another aspect of the present description relates to substituted thieno [3,2-d]pyrimidine compounds, forms, and pharmaceutical compositions there

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.

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.

Discovery of N-Substituted 3-Amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic Acids as Highly Potent Third-Generation Inhibitors of Human Arginase i and II

Recent efforts to identify new highly potent arginase inhibitors have resulted in the discovery of a novel family of (3R,4S)-3-amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid analogues with up to a 1000-fold increase in potency relative to the current standards, 2-amino-6-boronohexanoic acid (ABH) and N-hydroxy-nor-l-arginine (nor-NOHA). The lead candidate, with an N-2-amino-3-phenylpropyl substituent (NED-3238), example 43, inhibits arginase I and II with IC50 values of 1.3 and 8.1 nM, respectively. Herein, we report the design, synthesis, and structure-activity relationships for this novel series of inhibitors, along with X-ray crystallographic data for selected examples bound to human arginase II.

COMPOUNDS AND METHOD OF USE

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.

DIHYDROPYRROLOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER

The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 has any of the meanings hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and t

DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER

The present disclosure concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and R3 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cancer.

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.

SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-A]PYRAZIN-1 (2H)-ONE DERIVATIVES AS KINASE INHIBITORS

Compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 have any of the meanings defined hereinbefore in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cancer are disclosed.