1030613-07-0

Usage

Uses

Used in Pharmaceutical Industry:
Ethyl5-bromo-1,3,4-thiadiazole-2-carboxylate is used as a reactant/reagent for the preparation of hydroxyalkyl thiadiazole derivatives, which are known for their antibacterial properties. These derivatives can be utilized in the development of new antibiotics to combat bacterial infections, making Ethyl5-bromo-1,3,4-thiadiazole-2-carboxylate a valuable asset in the pharmaceutical industry.

Upstream product

• 540-80-7 tert.-butylnitrite 
• 64837-53-2 ethyl 5-amino-1,3,4-thiadiazole-2-carboxylate 

Downstream Products

• 933716-45-1 5-bromo-1,3,4-thiadiazole-2-carboxylic acid 
• 1339055-00-3 (5-bromo-1,3,4-thiadiazol-2-yl)methanol 

Relevant academic research and scientific papers

Development of a Scalable Route for a Key Thiadiazole Building Block via Sequential Sandmeyer Bromination and Room-Temperature Suzuki-Miyaura Coupling

To avoid the use and handling of Lawesson's reagent or other thiation agents in the in-house kilolab, a new scalable route to ethyl 5-(2,4-difluorophenyl)-1,3,4-thiadiazole-2-carboxylate (1) was developed. The key to success was the use of a commercially available amino-thiadiazole building block, which was converted into the desired product via a sequence of Sandmeyer bromination and Suzuki-Miyaura coupling. The different parameters of the Pd-catalyzed coupling have been studied in detail and allowed the reaction to be performed under mild conditions at room temperature and with low catalyst loading. The inconsistencies of the initial scale-up runs with regard to the sluggish conversion of the Suzuki-Miyaura coupling due to Cu contamination were addressed, and the findings were directly implemented in the subsequent batches, which finally led to an improved overall understanding and robustness of the process.

CARBALDEHYDE OXIMES AS BUTYRYLCHOLINESTERASE REACTIVATORS

The present invention relates to compounds for their use in the reactivation of butyrylcholinesterase. Such compounds are useful in the treatment or prevention of the intoxication with at least one organophosphorus nerve agent. The invention also relates

NITRONE COMPOUNDS AND USE THEREOF

The present invention relates to novel nitrone compounds of formula (I), wherein, A, A1, R1, R2, R3, R4 and n are as defined in the description. The present invention further relates to their preparation and use to protect crops against undesired phytopathogenic microorganisms, phytopathogenic fungi and pests such as nematodes.

CYCLIC SULFAMIDE COMPOUNDS AND METHODS OF USING SAME

The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.

AMIDINE SUBSTITUTED BETA - LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS

The present invention relates to novel β-lactam compounds of formula (I), their preparation and use. In particular, this invention relates to novel β-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.

IMIDAZOLE DERIVATIVES AS CYP17 INHIBITORS FOR THE TREATMENT OF CANCER

The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP 17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia

The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia has been limited by preclinical adverse events associated with inhibition of SCD in skin and eye tissues. To establish a therapeutic window, we embarked on designing liver-targeted SCD inhibitors by utilizing molecular recognition by liver-specific organic anion transporting polypeptides (OATPs). In doing so, we set out to target the SCD inhibitor to the organ believed to be responsible for the therapeutic efficacy (liver) while minimizing its exposure in the tissues associated with mechanism-based SCD depletion of essential lubricating lipids (skin and eye). These efforts led to the discovery of MK-8245 (7), a potent, liver-targeted SCD inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window.

HETEROCYCLIC FLAVIVIRIDAE VIRUS INHIBITORS

The invention is related to anti -viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful

NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE

Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and

NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE

Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desat- urase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.