454248-53-4

Usage

Uses

Used in Organic Synthesis:
Tert-Butyl (R)-4-Methyl-2,2-Dioxo-[1,2,3]Oxathiazolidine-3-Carboxylate is used as a reagent in organic synthesis for its ability to participate in various chemical reactions, contributing to the formation of complex organic molecules.
Used in Pharmaceutical Research:
In pharmaceutical research, Tert-Butyl (R)-4-Methyl-2,2-Dioxo-[1,2,3]Oxathiazolidine-3-Carboxylate is employed as a reagent to aid in the development of new drugs and biologically active compounds, leveraging its unique chemical properties.
Used in Metal-Containing Materials Production:
Tert-Butyl (R)-4-Methyl-2,2-Dioxo-[1,2,3]Oxathiazolidine-3-Carboxylate is used as a component in the production of metal-containing materials due to its capacity to form stable complexes with metal ions, which is valuable in creating materials with specific properties.
Used in Catalyst Development:
Tert-Butyl (R)-4-Methyl-2,2-Dioxo-[1,2,3]Oxathiazolidine-3-Carboxylate is also utilized in the development of catalysts, where its metal-ion complexing ability can enhance the efficiency and selectivity of catalytic processes in various chemical industries.
Used in the Development of New Drugs:
Due to its unique chemical structure and reactivity, Tert-Butyl (R)-4-Methyl-2,2-Dioxo-[1,2,3]Oxathiazolidine-3-Carboxylate has potential applications in the development of new drugs, where it may contribute to the creation of pharmaceuticals with novel mechanisms of action or improved therapeutic profiles.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 129991-09-9 (R)-N-Boc-2-aminobutane 
• 79069-13-9 (R)-2-tertbutoxycarbonylamino-1-propanol 

Downstream Products

• 1338090-90-6 [(R)-1-methyl-2-(3-trifluoromethylphenyl)ethyl]carbamic acid tert-butyl ester 
• 454248-61-4 (R)-4-methyl-1,2,3-oxathiazolidine 2,2-dioxide 
• 167421-83-2 tert-butyl N-[(1R)-1-methyl-2-phenylethyl]carbamate 
• 941596-59-4 5-benzyloxy-1-((R)-2-tert-butoxycarbonylamino-propyl)-1H-indole-2-carboxylic acid ethyl ester 
• 847199-90-0 tert-butyl (R)-(1-(1H-indol-3-yl)propan-2-yl)carbamate 

Relevant academic research and scientific papers

PROCESSES FOR MAKING SERD TRICYCLIC COMPOUNDS HAVING A SUBSTITUTED PHENYL OR PYRIDINYL MOIETY

Provided herein are processes for the preparation of compounds useful in the treatment of cancer.

Efficient Manufacturing Process for the Selective Estrogen Receptor Degrader GDC-9545 (Giredestrant) via a Crystallization-Driven Diastereoselective Pictet-Spengler Condensation

GDC-9545 is a selective estrogen receptor degrader that is being developed as a treatment for ER+/HER2- breast cancer. A robust, convergent manufacturing process for GDC-9545 was developed. The process features a Wenker aziridine synthesis to produce the key starting material tryptamine 11, a highly efficient C-N coupling between aminoazetidine 9 and 2,6-difluoro-4-bromobenzaldehyde diethyl acetal (33) to construct key intermediate 10, and a crystallization-driven diastereoselective Pictet-Spengler reaction to furnish the active pharmaceutical ingredient GDC-9545·tartrate.

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.

SELECTIVE ESTROGEN RECEPTOR DOWNREGULATORS AND USES THEREOF

The invention relates to novel tetrahydroisoquinoline compounds that are selective estrogen receptor downregulators (SERDs). The present invention also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and to the use of the compounds in the treatment of estrogen receptor (ER) mediated or dependent diseases or conditions, for example cancer such as breast cancer.

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.

Tricyclic Indazoles - A Novel Class of Selective Estrogen Receptor Degrader Antagonists

Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists. Replacement of a phenol, present in our previously reported tetrahydroisoquinoline scaffold, with an indazole group led to the removal of a reactive metabolite signal in an in vitro glutathione trapping assay. Further optimization, guided by X-ray crystal structures and NMR conformational work, varied the alkyl side chain and pendant aryl group and resulted in compounds with low turnover in human hepatocytes and enhanced chemical stability. Compound 9 was profiled as a representative of the series in terms of pharmacology and demonstrated the desired estrogen receptor α degrader-antagonist profile and demonstrated activity in a xenograft model of breast cancer.

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.

Synthesis of Chiral Tryptamines via a Regioselective Indole Alkylation

A practical synthesis of chiral tryptamines from simple, unprotected indoles has been developed. Indole nucleophiles prepared with MeMgCl in the presence of CuCl reacted with chiral cyclic sulfamidates almost exclusively at the C3-position of i

INDAZOLE DERIVATIVES THAT DOWN-REGULATE THE ESTROGEN RECEPTOR AND POSSESS ANTI-CANCER ACTIVITY

The specification relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.

MK2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.