Day: September 16, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.159635-49-1,tert-Butyl 4-methylenepiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Synthesis of tert-butyl 1,1-dichloro-2-oxo-7-azaspiro[3.5]nonane-7-carboxylate; Dry DME (8.0 L) and tert-butyl 4-methylenepiperidine-1-carboxylate (800 g, 4.06 mol) were charged to a reactor. Zinc-copper couple (800 g; CAS No.53801-63-1, Alfa-Aesar) was charged to the reactor, and the mixture was warmed to 34¡ã C. Trichloroacetyl chloride (1448 g, 8.0 mol, 888 mL) was added dropwise under a nitrogen atmosphere to the stirred suspension in the following manner: 80 mL of trichloroacetyl chloride was added. After 10 min, an exotherm elevated the reaction temperature to 39¡ã C. Dropwise addition of the remaining trichloroacetyl chloride was resumed immediately at a rate to maintain a temperature between 40-44¡ã C. using a 25¡ã C. jacket. After the addition was complete, the reaction was stirred at 40¡ã C. for 15 min. Cyclohexane (10 L) was added to the mixture. The mixture was filtered through a pad of celite, washing with cyclohexane (2 L). The filtrate was concentrated to approximately 3 L and then was diluted with MTBE (3 L) and cyclohexane (2 L) and filtered through a pad of magnesol (1 kg), washing with 1:1 cyclohexane/MTBE (3 L). The filtrate was washed with saturated potassium bicarbonate (3 L) and brine (2 L). The organic layer was filtered through a pad of silica gel (300 g) with a pad of magnesol (200 g) on top. The filtrated was concentrated to yield the title compound as an orange solid (1123 g, 91percent). 1H NMR (400 MHz, CDCl3) delta ppm 4.05-4.13 (m, 2H), 3.08 (s, 2H), 2.80-2.88 (m, 2H), 1.88-1.97 (m, 2H), 1.71-1.78 (m, 2H), 1.46 (s, 9H). m/z 252, 254 (MH+ minus t-Bu)., 159635-49-1

159635-49-1 tert-Butyl 4-methylenepiperidine-1-carboxylate 2756808, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Pfizer Inc.; US2010/113465; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

479630-08-5, 1-Boc-4-(2-Ethoxycarbonyl-acetyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 5 (15 g, 45 mmol) was dissolved in anhydrous ethanol (400 mL) with compound 6 (9.45 g, 49.5 mmol), followed by addition of trifluoroacetic acid (20 mL) and heating at 80 C for 12 hours. Cool to room temperature and spin the solvent. The reaction mixture was diluted with water (100 mL), extracted with 1 M NaOH, and extracted with ethyl acetate (3×200 mL). The extract was dried over anhydrous sodium sulfate, filtered and dried with methanol: dichloromethane = 1:20 Compound 7 (13. 82 g, 72%) was isolated.

479630-08-5, As the paragraph descriping shows that 479630-08-5 is playing an increasingly important role.

Reference£º
Patent; HU, XIANMING; HONG, XUECHUAN; WANG, HONGBO; ZHU, XI; DING, MINGMIN; L, GUANGYAO; ZHANG, JIANQIAO; WEN, MENG; QU, CHUNRONG; ZHU, JINMEI; (14 pag.)CN104292233; (2016); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1038866-44-2, Spiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazin]-2′(1’H)-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 581-(6-(7-methyl-2-(tetrahydrofuran-3-yl)-1H-benzo[d]imidazol-5-yloxy)pyrimidin-4-yl)spiro-[piperidin-4,4′-pyrido[2,3-d][1,3]oxazin]-2′(1’H)-one; 138 mg (0.54 mmol) spiro[piperidin-4,4′-pyrido[2,3-d][1,3]oxazin]-2′(1’H)-one hydrochloride, 180 mg (0.54 mmol) 5-(6-chloropyrimidin-4-yloxy)-7-methyl-2-(tetrahydrofuran-3-yl)-1H-benzo[d]imidazole and 280 muL (1.62 mmol) DIPEA in 5.0 mL DMF were stirred overnight at 60 C. The reaction mixture was combined with ice water. The precipitate formed was suction filtered and purified by chromatography. The fractions containing product were combined and evaporated down i.vac. to leave the aqueous residue. This was neutralised with an aqueous NaHCO3 solution and extracted with ethyl acetate. The organic phase was dried and evaporated down i.vac.Yield: 50 mg (18% of theory)ESI-MS: m/z=514 (M+H)+ Rt(HPLC): 2.88 min (method L)

1038866-44-2, As the paragraph descriping shows that 1038866-44-2 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2012/88755; (2012); 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.940890-90-4,(S)-tert-Butyl 3-((methylsulfonyl)oxy)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

3-(4-phenoxyphenyl) lH-pyrazolo [3,4-d] pyrimidin-4-amine (1.14g, 3.76mmol)was dissolved DMF (30mL) in, and then the reaction solution was added (S)-tert-butyl 3-((methylsulfonyl) oxy) piperidine-1-carboxylate (4.2g, 15.04mmol), cesium carbonate(0.64mL, 8.21 mmol), 4- dimethylaminopyridine pyridine (3.67g, 11.28mmol). Was stirredat 90 deg.] C 8h, the reaction was completed, distilled under reduced pressure of DMF,and extracted with dichloromethane (150mL ¡Á 3), brine (60mL), dried over anhydroussodium sulfate, the solvent was distilled off under reduced pressure, the crude productwas silica gel column Analysis of separation and purification (methylene chloride /methanol (V / V) = 40/1), to give the product (1.28g, 70percent)., 940890-90-4

The synthetic route of 940890-90-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangdong HEC Pharmaceutical Co., Ltd; LIU, BING; BAI, SHUN; ZHANG, YINGJUN; ZHENG, CHANGCHUN; YANG, TIPING; ZHOU, YOUBAI; (33 pag.)CN105399756; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.111153-74-3,1-Phenylpiperidine-4-carbaldehyde,as a common compound, the synthetic route is as follows.

Step E 4-[2-{1-(Triphenylmethyl)-4-imidazolyl}ethenyl]-1-phenylpiperidine The product from Step D is dissolved in THF and cooled to -78 C. under nitrogen. A solution of LDA in THF is added dropwise. The reaction was stirred at -78 C. for 1 h, then a solution of 4-formyl-1-phenylpiperidine from Step A is added, and the reaction warmed to room temperature overnight. The reaction is quenched with ammonium chloride solution, and extracted with ethyl acetate. The title compound is obtained after chromatography on silica gel.

111153-74-3, 111153-74-3 1-Phenylpiperidine-4-carbaldehyde 13842992, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Merck & Co., Inc.; US5891889; (1999); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.189442-92-0,1-Boc-4-Formyl-4-methylpiperidine,as a common compound, the synthetic route is as follows.

Step 3. Synthesis of 4-aminomethyl-1-t-butoxycarbonyl-4-methylpiperidine To a solution of 367 mg of N-t-butoxycarbonyl-4-methylpiperidine-4-carbaldehyde in 5 ml of methanol, 1.2 g of ammonium acetate and 130 mg of sodium cyanoborohydride, followed by stirring for 1 hour at room temperature. The reaction mixture was diluted with chloroform, washed sequentially with a 3N sodium hydroxide aqueous solution and brine, and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to give the title compound., 189442-92-0

189442-92-0 1-Boc-4-Formyl-4-methylpiperidine 22248051, apiperidines compound, is more and more widely used in various fields.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129888-60-4,tert-Butyl 3-((methylsulfonyl)oxy)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

[0373] Step1. A 20 mL vial fitted with a magnetic stir bar was charged with pyrimidine 1(303 mg), mesylate 9 (300 mg) (tert-Butyl3-(methylsulfonyloxy)piperidine-1-carboxylate (9) was prepared according toCosta, et al, J. Med. Chem. 1992, 35, 4334-4343), cesium carbonate (450 mg),and DMF (2 mL). The reaction mixture was heated to 50 C. and stirred for 3 d.The reaction mixture was diluted with water (20 mL) and extracted with EtOAc(3¡Á20 mL). The organic layers were combined, washed with water (3¡Á20 mL) andbrine (1¡Á20 mL). The organic layer was dried over Na2SO4, filtered, andconcentrated under reduced pressure. The resulting residue was redissolved inDCM (3 mL), and treated with TFA (1 mL) and water (0.5 mL). The reactionmixture was stirred for 5 minutes at room temperature and the solutionconcentrated under reduced pressure. The residue was treated with TFA (1 mL)and stirred for 5 minutes and concentrated twice more. The residue was thendiluted with EtOAc and washed with 5% NaHCO3. The organic layer was thenextracted with 1 M HCl. The acid washes were neutralized with NaOH andextracted with EtOAc. The resulting organic layer was dried over Na2SO4,filtered, and concentrated under reduced pressure. The resulting residue wasredissolved in DCM (5 mL) and combined with cyanoacetic acid (170 mg), HOBt(130 mg), DIPEA (0.2 mL), and EDC (250 mg). The reaction mixture was stirredovernight at room temperature. The reaction mixture was diluted with EtOAc,washed with 5% citric acid, followed by 5% NaHCO3, and then brine. The organiclayer dried over Na2SO4, filtered, and concentrated under reduced pressure. Theresulting residue was partially purified by Si-gel chromatography to give3-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperi-din-1-yl)-3-oxopropanenitrile (10) 156 mg (34% yield over 3 steps).

129888-60-4, 129888-60-4 tert-Butyl 3-((methylsulfonyl)oxy)piperidine-1-carboxylate 568122, apiperidines compound, is more and more widely used in various fields.

Reference£º
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.782501-25-1,1-Boc-4-Chlorosulfonylpiperidine,as a common compound, the synthetic route is as follows.

782501-25-1, A solution of tert-butyl 4-(chlorosulfonyl)piperidine-1-carboxylate (3.000 g, 10.572 mmol) in dichloromethane (50 mL) was mixed at the room temperature with 3-chloroaniline (1.618 g, 12.686 mmol) and triethylamine (2.210 mL, 15.858 mmol), and stirred at the same temperature for 18 hr. Then, water was added to the reaction mixture, followed by extraction with dichloromethane. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous Mg504, filtered, and concentrated in vacuo. The residue was chromatographed (5i02, 40 g cartridge; ethyl acetate / hexane = 20 % to 50 %) to give the concentrate, and then the concentrate was dissolved in ethyl acetate (10 mL) and hexane (100 mL) and stirred. The resulting precipitates were collected by filtration, washed by hexane, and dried to give tert-butyl 4-(N-(3-chlorophenyl)sulfamoyl)piperidine- 1-carboxylate as white solid(0.860 g, 21.7 %).

782501-25-1 1-Boc-4-Chlorosulfonylpiperidine 45789737, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; CHOI, Daekyu; MIN, Jaeki; BAE, Miseon; YANG, Hyunmo; KIM, Dohoon; (644 pag.)WO2017/18803; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

161491-24-3, 1-tert-Butyl 3-methyl 4-oxopiperidine-1,3-dicarboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In the reaction flask,N-Boc-3-carboxylate-4-piperidone 25 g (0.1 mol)Added to methanol 300mL,Ammonium acetate 22g (0.3 mol) was further added,Reaction overnight,TLC monitoring raw material reaction is complete, dry methanol, add water 900mL,The reaction mixture was extracted with 300 mL of dichloromethane three times,The combined organic phases were dried over anhydrous sodium sulfate,Dried to get a red oily liquidN-Boc-3- carboxylateAmino-3-ene-piperidine 25g

161491-24-3, As the paragraph descriping shows that 161491-24-3 is playing an increasingly important role.

Reference£º
Patent; Mao Jiajing; (22 pag.)CN107286160; (2017); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.625471-18-3,(S)-tert-Butyl 3-aminopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,625471-18-3

Amino derivative 43a (1.05 g, 5.24 mmol), 2,5-diamino-4,6-dichloropyrimidine 17 (1.03 g, 5.76 mmol), and triethylamine (3.1 ml, 22.53 mmol) were suspended in n-butanol (80 ml) and heated to 140 ¡ãC in a pressure vessel over 48 h. After the reaction was completed, the solvent was evaporated and the residue chromatographed on a silica gel using a linear gradient of ethyl acetate in toluene. The product was obtained in a 54percent yield (969 mg, 2.82 mmol) as a light orange foam.1H NMR, 13C NMR, and IR spectra were identical to those of 33b. HRMS (ESI) C14H24O2N6Cl (M+H)+ calcd 343.1644, found 343.1645; [alpha]D20 -31.1 (c 0.106, EtOH).

625471-18-3 (S)-tert-Butyl 3-aminopiperidine-1-carboxylate 1501975, apiperidines compound, is more and more widely used in various fields.

Reference£º
Article; Kovac?kova?, Son?a; Drac?i?nsky?, Martin; Rejman, Dominik; Tetrahedron; vol. 67; 7; (2011); p. 1485 – 1500;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem