78865-47-1

Upstream product

• 1729-67-5 Methyl 2,3-dibromopropionate 
• 156-57-0 2-mercaptoethylamine hydrochloride 
• 67-56-1 methanol 
• 114525-81-4 (R)-4-(tert-butoxycarbonyl)thiomorpholine-3-carboxylic acid 
• 18598-63-5 L-cysteine methyl ester hydrochloride 
• 1041173-31-2 1-vinyltetrahydro-1H-thiophenium trifluoromethanesulfonate 
• 872424-97-0 2-amino-3-(2-chloro-ethylsulfanyl)-propionic acid methyl ester hydrochloride 

Downstream Products

• 753027-50-8 4-(2-nitrobenzoyl)thiomorpholine-3-carboxylic acid methyl ester 
• 104053-55-6 3-phenyl-3-oxo-7-thia-1,3-diazabicyclo<4.3.0>nonane-2-thione 
• 104053-47-6 3-methoxycarbonyl-4-(N-phenylcarbamoyl)-1,4-tetrahydrothiazine 
• 49855-43-8 3-phenyl-7-thia-1,3-diazabicyclo<4.3.0>nonane-2,4-dione 

Relevant academic research and scientific papers

Synthesis and Separation of Diastereomers of Thiomorpholinecarboxylic Acid Esters

It is shown that the reaction of methyl 2,3-dibromopropionate with aminoethanethiol and L-cysteine methyl ester leads to the formation of esters of thiomorpholine-3-carboxylic and thiomorpholine-3,5-dicarboxylic acids; the latter ester was separated into individual diastereomers.

Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52

The FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Both proteins have been implicated in prostate cancer. Furthermore, single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders. Rapamycin and FK506 are two macrocyclic natural products that bind to these proteins indiscriminately but with nanomolar affinity. We here report the cocrystal structure of FKBP51 with a simplified α-ketoamide analogue derived from FK506 and the first structure-activity relationship analysis for FKBP51 and FKBP52 based on this compound. In particular, the tert-pentyl group of this ligand was systematically replaced by a cyclohexyl ring system, which more closely resembles the pyranose ring in the high-affinity ligands rapamycin and FK506. The interaction with FKBPs was found to be surprisingly tolerant to the stereochemistry of the attached cyclohexyl substituents. The molecular basis for this tolerance was elucidated by X-ray cocrystallography.

Synthesis of enantiopure 1,4-dioxanes, morpholines, and piperazines from the reaction of chiral 1,2-diols, amino alcohols, and diamines with vinyl selenones

The reactions of readily available vinyl selenones with enantiopure 1,2-diols, N-protected-1,2-aminoalcohols, and diamines gave substituted enantiopure 1,4-dioxanes, morpholines, and piperazines, respectively, in good to excellent yields. The same procedu

An annulation reaction for the synthesis of morpholines, thiomorpholines, and piperazines from β-heteroatom amino compounds and vinyl sulfonium salts

(Chemical Equation Presented) Heterocycling: Diphenyl vinyl sulfonium salt 1 acts first as an electrophile, then a base, and then again as an electrophile in this operationally simple, high yielding, one-pot synthesis of pharmacologically important morpholines, thiomorpholines, and piperazines. Compound 1 is an excellent synthon for the 1,2-ethane dication.

Substituted 6?membered n?heterocyclic compounds and their uses as neurological regulator

This invention relates to substituted 6-membered N-Herterocyclic neurotrophic compounds of formula (I) or pharmaceutically acceptable salts or hydrates thereof, wherein R1, R2, X, Y, and Z are as defined in the description; their pre