Category: 114525-81-4

(R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, A common heterocyclic compound, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route., 114525-81-4

Step a. Referring to Scheme 5-2, a mixture of compound 17 (667 mg, 2.4 mmol), (i^-N-Boc-thiomorpholine-S-carboxylic acid (594 mg, 2.4 mmol) and Et3N (486 mg, 4.8 mmol) in EtOAc (20 mL) was stirred at rt for 2h. Subsequently, the reaction mixture was concentrated and the residue was dried in vacuo to give crude compound 19, which was used for the next step without further purification. LC-MS (ESI): m/z 466.0 (M+Na)+.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. 114525-81-4. We look forward to the emergence of more reaction modes in the future.

Reference£º
Patent; PRESIDIO PHARMACEUTICALS, INC.; LI, Leping; ZHONG, Min; WO2010/65668; (2010); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

(R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, A common heterocyclic compound, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route., 114525-81-4

To a 100 mL round bottom flask, Intermediate 15 (1.28 g, 3.28 mmol), Intermediate 9 (0.81 g, 3.28 mmol), EDCI (0.94 g, 4.92 mmol), HOBt (0.66 g, 4.92 mmol), DIEA (0.85 g, 6.56 mmol) and tetrahydrofuran (40 mL) were added, and stirred at room temperature overnight. Thereafter, the reaction product was subjected to vacuum distillation for removal of solvent, dissolved with water, and extracted 3 times with ethyl acetate. The extracts were combined, washed 3 times with saturated brine, concentrated, and separated through a silica gel column (eluent: ethyl acetate/methanol/ammonia), to give 1.63 g of a white foamy solid product, yield 80.5%. [0091] 1H-NMR (400 MHz, CDCl3) delta ppm: 8.77 (1H, m), 8.02 (1H, m), 7.43 (1H, m), 7.31 (1H, m), 7.20 (1H, m), 7.05 (1H, m), 6.56 (1H, m), 4.85 (2H, d, J = 5.2 Hz), 4.02-3.44(10H, brm), 3.13 (1H, m), 2.83 (2H, m), 2.44 (2H, m), 2.02 (9H, s); EI-MS (m/z): 618.2 [M+H]+.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. 114525-81-4. We look forward to the emergence of more reaction modes in the future.

Reference£º
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; Peking University; LI, Song; WANG, Ying; XIAO, Junhai; MA, Dalong; GONG, Hongwei; QI, Hui; WANG, Lili; LING, Xiaomei; ZHENG, Zhibing; ZHANG, Yang; ZHONG, Wu; LI, Meina; XIE, Yunde; XU, Enquan; LI, Xingzhou; MA, Jing; ZHAO, Guoming; ZHOU, Xinbo; WANG, Xiaokui; LIU, Hongying; EP2805947; (2014); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 114525-81-4, name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows. 114525-81-4

To a 100 mL round bottom flask, Intermediate 15 (1.28 g, 3.28 mmol), Intermediate 9 (0.81 g, 3.28 mmol), EDCI (0.94 g, 4.92 mmol), HOBt (0.66 g, 4.92 mmol), DIEA (0.85 g, 6.56 mmol) and tetrahydrofuran (40 mL) were added, and stirred at room temperature overnight. Thereafter, the reaction product was subjected to vacuum distillation for removal of solvent, dissolved with water, and extracted 3 times with ethyl acetate. The extracts were combined, washed 3 times with saturated brine, concentrated, and separated through a silica gel column (eluent: ethyl acetate/methanol/ammonia), to give 1.63 g of a white foamy solid product, yield 80.5%.1H-NMR (400 MHz, CDCl3) delta ppm: 8.77 (1H, m), 8.02 (1H, m), 7.43 (1H, m), 7.31 (1H, m), 7.20 (1H, m), 7.05 (1H, m), 6.56 (1H, m), 4.85 (2H, d, J=5.2 Hz), 4.02-3.44 (10H, brm), 3.13 (1H, m), 2.83 (2H, m), 2.44 (2H, m), 2.02 (9H, s); EI-MS (m/z): 618.2 [M+H]+.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant. 114525-81-4, we look forward to future research findings about .

Reference£º
Patent; Li, Song; Wang, Ying; Xiao, Junhai; Ma, Dalong; Gong, Hongwei; Qi, Hui; Wang, Lili; Ling, Xiaomei; Zheng, Zhibing; Zhang, Yang; Zhong, Wu; Li, Meina; Xie, Yunde; Xu, Enquan; Li, Xingzhou; Ma, Jing; Zhao, Guoming; Zhou, Xinbo; Wang, Xiaokui; Liu, Hongying; US2015/126500; (2015); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 114525-81-4, Name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, molecular formula is C10H17NO4S

Optically active thiomorpholine derivatives

Optically active carboxamide derivatives having analgesic activity and being useful as an analgesic agent. The compounds have a general formula: STR1 (in the above formula, R1 represents a hydrogen or halogen atom; R2 represents a halogen atom; R3 represents a pyrrolidino or piperidino group; Y represents a methylene or carbonyl group; and n is an integer of 1 or 2) and pharmacologically acceptable salts thereof.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. category: Thiomorpholine, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 114525-81-4

Design and synthesis of a series of pyrido[2,3-d]pyrimidine derivatives as CCR4 antagonists

A series of pyrido[2,3-d]pyrimidine derivatives were designed and synthesized based on known CC chemokine receptor 4 (CCR4) antagonists. The activities of all the newly synthesized compounds were evaluated using a chemotaxis inhibition assay. Compound 6b was proven to be a potent CCR4 antagonist that can block cell chemotaxis induced by macrophage-derived chemokine (MDC), thymus and activation regulated chemokine (TARC), and CKLF1, the natural ligands of CCR4. In addition, compound 6b is more effective than budesonide in the murine rhinitis model. The intravenous injection LD 50 of compound 6b is 175 mg/kg and the oral LD50 is greater than 2,000 mg/kg.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Synthetic Route of 114525-81-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.114525-81-4, Name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, molecular formula is C10H17NO4S. In a Article£¬once mentioned of 114525-81-4

Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes. The pharmacologic utility of TGR5 agonists has been limited by systemic target-related effects such as excessive gallbladder filling and blockade of gallbladder emptying. Gut-restricted TGR5 agonists, however, have the potential to avoid these side effects and consequently be developed into drugs with acceptable safety profiles. We describe the discovery and optimization of a series of gut-restricted TGR5 agonists that elicit a potent response in mice, with minimal gallbladder-related effects. The series includes 12 (TGR5 EC50: human, 143 nM; mouse, 1.2 nM), a compound with minimal systemic availability that may have therapeutic value to patients with type 2 diabetes mellitus, nonalcoholic steatohepatitis, or inflammatory bowel disease.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In an article, published in an article,authors is , once mentioned the application of Computed Properties of C10H17NO4S, Name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid,molecular formula is C10H17NO4S, is a conventional compound. this article was the specific content is as follows. Computed Properties of C10H17NO4S

INHIBITORS OF HCV NS5A

Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Computed Properties of C10H17NO4S, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about Computed Properties of C10H17NO4S

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.C10H17NO4S, introducing its new discovery. , Recommanded Product: 114525-81-4

Inhibitors of &alpha4&beta1 mediated cell adhesion

The present invention relates to compound of formula (I), that are potent inhibitors of alpha4beta1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing alpha4beta1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Application of 114525-81-4, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid,introducing its new discovery.

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 alpha-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.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Related Products of 114525-81-4, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid,introducing its new discovery.

MODULATORS OF THE G PROTEIN-COUPLED MAS RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complications resulting from elevated blood pressure and/or reduced tissue perfusion

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem