Month: March 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.14813-01-5,1-Benzylpiperidin-3-ol,as a common compound, the synthetic route is as follows.

Step 1: To a stirred solution of [5] (l .Og, 5.2mmol) in DCM (20.0ml) was added TEA (1.9g, 15.2mmol) at room temperature. After an additional stirring for 5 minutes at same temperature, Mesyl chloride (0.55ml, 7.8mmol) was added. The reaction temperature was allowed to stirred at this temperature for 3h. TLC showed complete consumption of starting material. Water (100 ml) was added and organic layer was extracted with ethyl acetate (2 x 100 ml). The combined organic layers were washed with water, brine and dried over sodium sulphate. The organic layer was concentrated to afford light brown sticky material [9] which was used further without any purification (l.lg, 78%).Analytical Data: [9]ESIMS: 270 [M++l]., 14813-01-5

14813-01-5 1-Benzylpiperidin-3-ol 85773, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; SPHAERA PHARMA PVT. LTD.; DRUG DISCOVERY RESEARCH CENTRE; DUGAR, Sundeep; MAHAJAN, Dinesh; RAI, Santosh Kumar; RAO, Kanury; SINGH, Varshneya; WO2015/181837; (2015); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

236406-22-7, 1-Boc-4-(Aminomethyl)-4-methylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 6. Synthesis of 4-benzyloxycarbonylaminomethyl-1-{(2R)-2-((1R)-3,3-difluorocyclopentyl)-2-hydroxy-2-phenylacetyl}-4-methylpiperidine The title compound was prepared by a method similar to Step 3 for Example 1, using 4-benzyloxycarbonylaminomethyl-4-methylpiperidine.

236406-22-7, As the paragraph descriping shows that 236406-22-7 is playing an increasingly important role.

Reference：
Patent; Banyu Pharmaceutical Co Ltd; US6140333; (2000); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

20691-89-8, 1-Methyl-4-piperidinemethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 7-fluoro-6-methoxy-4-oxo-1,4-dihydro-3-quinolinecarbonitrile (1.5 g, 6.9 mmol) and (1-methylpiperidin-4-yl)-methanol (1.8 g, 13.7 mmol) (WO 200471212) and a 60% dispersion in mineral oil of sodium hydride (0.8 g, 34.4 mmol) is heated at 110 C. for 2 hours. The reaction mixture is quenched with methanol, concentrated, and azeotroped with toluene to give 2.25 g of a brown solid. A mixture of this solid and phosphorous oxychloride (15 mL, 159 mmol) is heated at reflux for 30 minutes then concentrated in vacuo. The residue is partitioned between aqueous sodium bicarbonate and methylene chloride. The organic layer is dried over sodium sulfate, filtered and concentrated on to silica gel. Purification by column chromatography eluting with a gradient of 1:9 methanol:methylene chloride to 0.05:1:5 triethylamine:methanol:methylene chloride provided 1.6 g of 4-chloro-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinoline-3-carbonitrile, mp 166-168 C. [0351] MS 346 (M+H)+ [0352] Analysis for C18H20ClN3O2-1 HCl+0.5 H2O [0353] Calcd: C, 54.72; H, 5.54; N 10.50. [0354] Found: C, 54.72; H, 6.07; N 10.05., 20691-89-8

The synthetic route of 20691-89-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Wyeth Holdings Corporation; US2003/212276; (2003); 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.7006-50-0,4-(Methylamino)-1-benzylpiperidine,as a common compound, the synthetic route is as follows.,7006-50-0

Preparation 21; N-(1-Benzy(piperidin-4-yl)-N-methyipyridin-2-amine A mixture of 4-methylamino-1-benzylpiperidine; [(1.5g, 6.2mmol), J. Med. Chem. 39, 3769-89; 1996] 1-bromopyridine (0.98g, 6.2mmol), sodium tert-butoxide (0.68g, 7.3mmol), 1,3-bis(diphenylphosphino)propane (102mg, 0.24mmol) and tris (dibenzylideneacetone)dipalladium(O) (113mg, 0.12mmol) in toluene (20mL) was heated under reflux for 4 hours. Tlc analysis showed that there was still starting material present and so further bromopyridine (0.49g, 3.1 mmol), tris (dibenzylideneacetone)dipalladium(0) (113mg, 0.12mmol), bis(diphenylphosphino)propane (102mg, 0.24mmol) and sodium tert-butoxide (0.68g, 7.3mmol) were added and heating continued for a further 3 hours. The mixture was then diluted with dichloromethane and washed with brine. The organic solution was dried over magnesium sulfate and concentrated in vacuo and the residue was purified by column chromatography on silica gel, eluting with dichloromethane: methanol: 0. 88 ammonia, 90: 10:1 to afford the title compound in 40% yield, 0.69g.

7006-50-0 4-(Methylamino)-1-benzylpiperidine 4136128, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; PFIZER LIMITED; PFIZER INC.; WO2005/105779; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

929252-65-3, tert-Butyl 4-(((4-(4-amino-2-fluorophenoxy)-6-methoxyquinolin-7-yl)oxy)methyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,929252-65-3

Step 1: preparation of tert-butyl 4-[[4-[2-fluoro-4-[[1-[(4-fluorophenyl) aminocarbonyl]cyclopropanecarbonyl]amino]phenoxy]-6-methoxyl-7-quinolyl] oxymethyl]piperidine-1-carboxylate: a mixture of intermediate C (1.5 g or 3.0 mmol), intermediate D (1.7 g or 7.6 mmol), DIPEA (1.55 g or 12.0 mmol), HATU (2.3 g or 6.0 mmol), DMAP (0.183 g or 1.5 mmol) in DMF (60 mL) is stirred at 30-40 C overnight. The mixture is concentrated under reduced presure, and the residue is purified by column chromatography (eluent: 1-5% MeOH in DCM) to obtain 1.9 g target compound (yield: 90%). The analytical data of the obtained product are as follows: mass spectrum m/z: 703.30 [M+H].

The synthetic route of 929252-65-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Beijing Konruns Pharmaceutical Co., Ltd.; YUN, Ziwei; WANG, Hongtao; EP2669289; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

61995-20-8, Benzyl 3-oxopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

61995-20-8, General procedure: The reaction mixture containing 200 mM substrate, 1mM NAD+, 5% (v/v) 2-propanol and 10mg crude enzyme READH in 1mL potassium phosphate buffer (100mM, pH 7.0) was incubated at 50 C. For ChKRED20, 40% (v/v) 2-propanol and a reaction temperature of 40 C were applied instead. The reaction was monitored by TLC, and terminated by extracting with methyl tert-butyl ether (1 mL). The organic extract was dried over anhydrous sodium sulfate and concentrated. The samples were subjected to chiral HPLC to determine the conversion and enantiomeric excess. The products were purified by silica gel column chromatography, and identified by NMR analysis, optical rotation measurements and mass spectrometry.

61995-20-8 Benzyl 3-oxopiperidine-1-carboxylate 1514169, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Li, Chao; Liu, Yan; Pei, Xiao-Qiong; Wu, Zhong-Liu; Process Biochemistry; vol. 56; (2017); p. 90 – 97;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1019351-46-2,Methyl 4-aminopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

200 g of tetrahydrofuran was placed in a 500 ml four-necked flask equipped with a stirring and a thermometer.12.5 g (0.05 mol) of (2S,5R)-5-benzyloxyaminopiperidine-2-carboxylic acid, 50 g of tri-n-butylamine,0.1 g of N,N-dimethylformamide, cooled at -10 C,A mixed solution of 23.8 g (0.08 mol) of solid phosgene and 80 g of tetrahydrofuran was added dropwise.The reaction was stirred at 10-20 C for 4 hours.Between 10 and 20 C, a mixed solution of 11.0 g (0.07 mol) of 1-methoxycarbonyl-4-aminopiperidine and 30 g of tetrahydrofuran was added.Stir the reaction between 15-20 C for 3 hours.The reaction liquid was poured into 300 g of ice water mixture and layered.The aqueous layer was extracted twice with dichloromethane, 50 g each time.The organic phases were combined and washed twice with saturated sodium chloride solution, 20 g each time.After the obtained organic phase recovers the solvent,18.2 g of (2S,5R)-N-(1-(methoxycarbonyl)piperidin-4-yl)-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide ,The liquid phase purity was 99.8%, and the yield was 93.3%., 1019351-46-2

The synthetic route of 1019351-46-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Xin Fa Pharmaceutical Co., Ltd.; Qi Yuxin; Li Xinfa; Wang Baolin; Xu Xin; Zhao Yinlong; Teng Yuqi; (9 pag.)CN109928970; (2019); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem