81569-57-5

Upstream product

• 72850-76-1 ethyl 2-amino-4-isopropyl-1,3-thiazole-5-carboxylate 
• 81569-67-7 2-bromo-4-methyl-3-oxo-pentanoic acid ethyl ester 
• 7152-15-0 ethyl 4-methyl-3-oxo-pentanoate 
• 115-08-2 thiocarboxamide 
• 35391-60-7 ethyl 2-chloro-4-methyl-3-oxopentanoate 

Downstream Products

• 261710-81-0 5-(hydroxymethyl)-4-isopropyl-thiazole 
• 72632-66-7 4-(propan-2-yl)-1,3-thiazol-5-amine 
• 261710-80-9 4-(1-methylethyl)thiazole-5-carboxaldehyde 
• 81569-42-8 4-isopropylthiazole-5-carboxylic acid 

Relevant academic research and scientific papers

Synthetic method of drug intermediate sulfur-containing nitrogen heterocyclic amine compound (by machine translation)

To the invention, 4 -N-BOC -3 - isopropylthiazole is obtained by reaction of 2 - methyl -4 - oxo-pentanoic acid ethyl ester, dichloromethane and sulfonyl chloride as a raw material, and then -3 - N-BOC - 2 - isopropylthiazole and HCl are added in the presence of ethanol as a solvent to obtain -4 - N-BOC-n-isopropythiazol -5 - methyl 4 -isoprop -5 -aminothiazole in the presence of triethylamine, and a NaOH solution is added as a solvent and then subjected to extraction washing to obtain 4 -yl -5 -aminothiazolethyl acetate in the presence of trifluoroethanol as a solvent and ethanol as a solvent to obtain ethyl acetate 4 - 5-propyl thiazole -5 - formic acid ethyl ester with ethanol as a 4 - solvent and an aqueous solution of N-BOC-5 n-isopropylthiazole 4 - and the like 4 -5 . The method has the advantages of clear steps, less waste, high yield, raw material saving and easy operation. (by machine translation)

HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS

ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS

The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.

Dehydroamino acids

Compounds of formula 1 and 1-1, wherein R1 is hydrogen, hydroxy, amino or halogen, R2 is hydrogen, hydroxy, or halogen and R3 is hydrogen (Formula 1) or R1 is hydrogen and R2 and R3 taken together with the ethenylene group connecting them form phenyl, pyrrole, pyrroline, oxopyrroline, pyrazole, triazole, or imidazole (Formula 1-1), A is R4 R5 are hydrogen, methyl, ethyl or halogen except that R4 r5 cannot both be hydrogen; and 1) B is hydrogen, or lower alkyl; or 2) B is where R6 R7 R8 and R9 are independently hydrogen, hydroxy, aminosulfonyl, halogen, lower alkoxy, cyano, amino, lower alkyl, lower alkyl amino, or nitro; or 3) B is where R10 is hydrogen, hydroxy, halogen, or lower alkyl and C is a five- or six- membered ring with 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur, which ring may be unsubstituted or mono- or di- substituted with lower alkyl, cycloalkyl, amino, or substituted amino; 4) B is where X and Y are independently methylene or nitrogen; or 5) B is where at leat one of T, U, V, or W is nitrogen, and any of T, U, V or W which is carbon may be substituted with lower alkyl, lower alkyl amino, lower alkoxy, hydroxy, aminosulfonyl, halogen, cyano, amino, or nitro; or 6) B is where Y is carbon or nitrogen; or 7) B is a five-membered aromatic ring with 1 to 3 heteratoms selected from nitrogen, oxygen, and sulfur which ring may be unsubstituted or mono- or di-substituted with lower alkyl, cycloalky, trifluoroloweralkyl, amino, halogen, substituted amino, or which ring may be fused with a 5 or 6 membered aromatic ring containing 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur; and pharmaceutically acceptable salts thereof, and related prodrugs, pharmaceutical compositions and methods of treatment, which compounds are useful for treating psoriasis.

Syntheses and Reactions of 2-Halo-5-thiazolecarboxylates

A variety of 2-halo-5-thiazolecarboxylates was prepared from substituted-3-aminoacrylates and 3-ketoesters.Selective reduction of 2-chloro-5-thiazolecarboxylates 4a, 4i and 4j with sodium borohydride in ethanol provided the corresponding 2-halo-5-thiazolemethanols 27 - 29.Nucleophilic displacement on methyl methanesulfonate (32c) occured selectivity at the 5-substituent to provide 2-chloro-4-(trifluoromethyl)-5-(heteroatom-substituted methyl)thiazoles 32d-f.

The Preparation of Thiazole-4- and -5-carboxylates, and an Infrared Study of their Rotational Isomers

Convenient general procedures have been developed for preparing series of thiazole-4- and -5-carboxylates containing alkyl and halogeno substituents.While both series of esters show i.r. carbonyl doublets caused by rotational isomerism, the more intense absorptions of the 4-carboxylates are the lower wavenumber components, whereas those of the 5-carboxylates are the higher wavenumber components.In both series the stronger bands arise from the thermochemically more stable forms; identification of these forms as the carbonyl O,S-syn-s-trans rotamers is more certain with the 4-carboxylates than with the 5-carboxylates.