Category: 143900-44-1

Chemistry is traditionally divided into organic and inorganic chemistry. Formula: C10H19NO3. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 143900-44-1

DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS

Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Formula: C10H19NO3, you can also check out more blogs about143900-44-1

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Piperidine – Wikipedia,
Piperidine | C5H14617N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ Product Details of 143900-44-1, Which mentioned a new discovery about 143900-44-1

Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR

Targeting acquired drug resistance represents the major challenge in the treatment of EGFR-driven non-small-cell lung cancer (NSCLC). Herein, we describe the structure-based design, synthesis, and biological evaluation of a novel class of covalent EGFR inhibitors that exhibit excellent inhibition of EGFR-mutant drug-resistant cells. Protein X-ray crystallography combined with detailed kinetic studies led to a deeper understanding of the mode of inhibition of EGFR-T790M and provided insight into the key principles for effective inhibition of the recently discovered tertiary mutation at EGFR-C797S.

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143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 57[0363] Synthesis of (^)-l-(3-(7H-pyrrolo[2,3-J]pyrirnidin-4-yloxy)piperidin- chloro-5-fluorophenylamino)ethanone.Reagents and conditions: a) NaH, DMSO, 4-chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H- pyrrolo[2,3-J]pyrimidine; b) TBAF, THF, reflux, 5 h; c) HC1 in 1 ,4-dioxane, rt, 30 min; d) EDCI, HOBt, 2-(3-chloro-5-fluorophenylamino)acetic acid, DMF, rt, 24 h.[0364] Synthesis of (S^-tert-butyl 3-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H- pyrrolo[2,3-J]pyrimidin-4-yloxy)piperidine-l-carboxylate: To a solution of (^-ieri-butyl 3- hydroxypiperidine-l-carboxylate (0.4 g, 2.0 mmol) in DMSO (5 mL) under nitrogen, was added NaH (60% suspension in mineral oil, 79 mg, 2.0 mmol). After the reaction was stirred for 1.5 h at rt, a solution of 4-chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-J]pyrimidine (564 mg, 2.0 mmol) in DMSO (5 mL) was added dropwise at rt and the mixture was heated at 50 C for 2h. The reaction mixture was cooled to rt, diluted with water (10 mL) and extracted with EtOAc (4 x 60 mL). The combined organic layer was washed with water (50 mL), dried over Na2S04 and concentrated in vacuo to give the crude compound which was purified by column chromatography (silica gel, gradient EtOAc in Hexanes) to give (750 mg, 85%) of the titled intermediate., 143900-44-1

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Patent; BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian, T.; SCOTT, Daniel; CONLON, Patrick; JENKINS, Tracy, J.; POWELL, Noel; GUAN, Bing; CURERVO, Julio, H.; WANG, Deping; TAVERAS, Art; WO2012/58645; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,143900-44-1

Step 3. To a stirred mixture of 3-iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine (5.9 g, 22.6 mmol, 1.00 equiv), (S)-tert-butyl 3-hydroxypiperidine-1-carboxylate (10 g, 50 mmol, 2.2 equiv) and triphenylphosphine (11.8 g, 45 mmol, 2.0 equiv) in tetrahydrofuran (300 mL) at 10 C. was added a solution of diisopropyl azodicarboxylate in tetrahydrofuran (30 mL) dropwise in 30 min. The resulting mixture was stirred at room temperature for 12 h and then concentrated under vacuum. The residue was purified on a silica gel column eluted with dichloromethane/methanol (100/1) to give 3 g (33%) of (R)-tert-butyl 3-(4-amino-3-iodo-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate as yellow solid.

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Patent; Taunton, JR., John William; Brameld, Kenneth Albert; Goldstein, David Michael; Mcfarland, Jesse; Krishnan, Shyam; Choy, Jonathan; US2014/323464; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Diisopropyl diazodicarboxylate (DAID, 1.2 ml) was added to a solution of 1-tert-butyloxycarbonyl-3-(S)-hydroxypiperidine ( 1.0 g,) and triphenylphosphine (2.59g) in tetrahydrofuran (50.0ml). To the resulting yellow solution, 3-(p-phenoxyphenyl)-1,2,5,7-tetraza-1H-inden-4-ylamine (1.0g). was added and warmed till dissolution, and stirred overnight at room temperature. The reaction mixture was filtered and the solvent was distilled under vacuum to get an oily residue, which was further purified by flash chromatography (30-50 % ethyl acetate/ hexane) on silicagel to give 0.3 g (0.3 w/w) of tert-butyloxycarbonyl-(1S)-1-[(3R)-3-piperidyl]-3-(p-phenoxyphenyl)-1,2,5,7-tetraza-1H-inden-4-ylamine as a light brown solid. The resulting solid was dissolved in dichloromethane (5 ml) and trifluoroacetic acid (0.6 ml) was added to it. After completion of reaction, water was added to reaction mass, followed by addition of methyl tert-butyl ether (20.0 ml). The layers were separated and the aqueous layer was basified with potassium carbonate and extracted with dichloromethane (15.0 ml x 2). The organic layer dried over sodium sulfate, filtered and evaporated to yield 0.2 g (0.6 w/w) of title compound as light yellow oil., 143900-44-1

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Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; ARUL, Ramakrishnan; SARIN, Gurdeep Singh; WAS, Sandeep; KUMAR, Vishal; (26 pag.)WO2017/163257; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (S)-1 -Boc-3-hydroxypiperidine (10.0 g, 49.7 mmol) and triethylamine (7.82 mL, 54.7 mmol in DCM (60 mL) under a nitrogen atmosphere, cooled at 0 ¡ãC, was added dropwise methanesulfonyl chloride (4.23 mL, 54.7 mmol). The mixture stirred for 1 h, diluted with water (60 mL) before being passed through a hydrophobic frit. The organic layer was concentrated under reduced pressure to afford fe/ -butyl (3S)-3-methylsulfonyloxypiperidine-1 -carboxylate (13.9 g, 49.7 mmol, 100percent yield) as a colourless solid. H-NMR (400 MHz, DMSO-c/6): delta (ppm) 4.76-4.71 (m, 1 H, CH), 3.69-3.66 (m 1 H), 3.65-3.60 (m, 1 H), 3.49-3.43 (m, 1 H), 3.37-3.31 (m, 1 H), 3.07 (s, 3H, CH3), 2.02-1 .96 (m, 1 H), 1 .94-1 .91 (m, 1 H), 1 .87- 1 .80 (m, 1 H), 1 .59-1 .53, 1 .48-1 .45 (m, 9H), 143900-44-1

The synthetic route of 143900-44-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; REDX PHARMA LIMITED; ARMER, Richard; BINGHAM, Matilda; MORRISON, Angus; CARSWELL, Emma; ELUSTONDO, Fred; WALKER, Rolf; GUISOT, Nicolas; LUCAS, Catherine; WO2014/188173; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred mixture of 3-iodo-lH-pyrazolo[3,4-d]pyrimidin-4-amine (5.9 g, 22.6 mmol, 1.00 equiv), (S)-tert-butyl 3-hydroxypiperidine-l -carboxylate (lOg, 50 mmol, 2.2 equiv) and triphenylphosphine (1 1.8g, 45 mmol, 2.0 equiv) in tetrahydrofuran (300 mL) at 10 C was added a solution of diisopropyl azodicarboxylate in tetrahydrofuran (30 mL) dropwise in 30 min. The resulting mixture was stirred at room temperature for 12 h and then concentrated under vacuum. The residue was purified on a silica gel column eluted with dichloromethane/methanol (100/1) to give 3g of (R)-tert-butyl 3-(4-amino-3-iodo-lH- pyrazolo[3,4-d]pyrimidin-l-yl)piperidine-l-carboxylate as a yellow solid.

143900-44-1, 143900-44-1 (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate 1514399, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; PRINCIPIA BIOPHARMA INC.; OWENS, Tim; VERNER, Erik; WO2014/39899; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.143900-44-1,(S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

(S)-tert-butyl 3-(tosyloxy)piperidine-1-carboxylate: To a stirred solution of (S)-tert-butyl 3-hydroxypiperidine-1-carboxylate (50 g, 1.0 eq), TsC1 (4-methylbenzene-1- sulfonyl chloride, 52 g, 1.1 eq) and DMAP (4-dimethylamiopryidine, 2.5g) in 500 mL CH2C12 at 0 C was added Et3N (51 g, 2.0 eq). After addition was completed, the reaction mixture was warmed to r.t. and stirred at that temperature for 40 hours. The organic layer was washed with water and brine, dried with anhydrous Na2SO4, and purified by flash chromatography to give the product as a white solid (80 g, 9 1%). ?H NMR (400 MHz, CDC13) oe 7.80 (d, J = 8.0 Hz, 2H), 7.34 (d, J = 8.0 Hz, 2H), 4.46 (brs, 1H), 3.54-3.58 (m, 1H), 3.31-3.40 (m, 3H), 2.45 (s, 3H), 1.80-1.88 (m, 1H), 1.65-1.79 (m, 2H), 1.47-1.52 (m, 1H), 1.43 (s, 9H).

143900-44-1, The synthetic route of 143900-44-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CENTAURUS BIOPHARMA CO., LTD.; HAN, Yongxin; YU, Rong; WANG, Zanping; LIANG, Zhi; HU, Quan; ZHU, Li; HU, Yuandong; SUN, Yinghui; ZHAO, Na; PENG, Yong; ZHAI, Xiaofeng; LUO, Hong; XIAO, Dengming; WO2014/82598; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem