Month: March 2022

10338-57-5, 4-(Piperidin-1-yl)benzaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 4-morpholinobenzaldehyde (1 mmol, 0.191 g) was added to a stirred mixture of malononitrile (1.5 mmol, 0.099 g), and catalytic amount of SSC NPs (0.012 g, 2 mol%) in ace-tonitrile (10 mL). It was allowed to the mixture to stir at 70 C under sonication about 25-60 minutes. After completion of the reaction (the reaction progress was monitored by TLC using EtOAc/n-hexane (1:1) as eluent), the reaction mixture was filtered to separate precipitate. Next, the pre-cipitate was dissolved in boiling ethanol and then was fil-trated to separate catalyst. Finally, pure crystalline product was obtained from filtrate. Since the catalyst is reusable, at the end of the reaction, it was washed by boiling methanol three times (3 × 2 mL), dried at 90 C for 2 h and re-used in further cycles. Also, in the following, we explain more details about reusability results of the catalyst on model reaction., 10338-57-5

The synthetic route of 10338-57-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Pourshojaei, Yaghoub; Nikzad, Maryam; Eskandari, Khalil; Darijani, Mohammad-Hossein; Hassanzadeh, Abdolreza; Faghih-Mirzaei, Ehsan; Asadipour, Ali; Croatica Chemica Acta; vol. 91; 1; (2018); p. 19 – 28;,
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, b) 18.9 mug of 1-benzyl-4-methylaminopiperidine as the oil prepared according to a) are taken up in 250 ml of methanol and combined with 8.3 g of cyclopropanecarboxaldehyde and 11.3 g of sodium cyanoborohydride. The mixture is stirred for 5 hours at 40-50 C., then for about another 16 hours at ambient temperature. It is then acidified with 2 N hydrochloric acid, evaporated to dryness in vacuo and the residue is taken up in water. It is washed with ether, made alkaline with concentrated sodium hydroxide solution and extracted with ether/ethyl acetate. The organic extract is dried over sodium sulphate and freed from the solvents in vacuo. 22.7 g 1-benzyl-4-(cyclopropylmethyl-methyl-amino)-piperidine are obtained as a yellowish oil.

The synthetic route of 7006-50-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Boehringer Ingelheim Pharma GmbH & Co. Kg; US2005/148562; (2005); 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.62718-31-4,1-Benzylpiperidine-4-carbonitrile,as a common compound, the synthetic route is as follows.

62718-31-4, Step 1. Synthesis of 1-benzyl-4-ethylpiperidine-4-carbonitrile The title compound was prepared by a method similar to Step 2 for Example 3, using 1-benzylpiperidine-4-carbonitrile and ethyl iodide.

62718-31-4 1-Benzylpiperidine-4-carbonitrile 793383, apiperidines compound, is more and more widely used in various fields.

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

5810-56-0,5810-56-0, 4-Acetamidopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

21.1 c N-(1-{4-[2-(4-Benzyloxy-6-oxo-6H-pyridazin-1-yl)-ethyl]-benzyl}-piperidin-4-yl)-acet- amideTo 125 mg (0.31 mmol) 5-benzyloxy-2-[2-(4-bromomethyl-phenyl)-ethyl]-2/-/-pyridazin-3-one (example 21.1 b) in 2.0 ml. DMF is added at RT 89 mg (0.63 mmol) lambda/-piperidin-4-yl- acetamide and 109 mul_ (0.63 mmol) N-ethyl-diisopropylamine. The reaction mixture is stirred 1 h at RT and is directly transferred to reverse HPLC purification (Waters symmetry, C18; water (0.15 % formic acid)/acetonitrile 95:5 to 5:95). Yield: 107 mg (74% of theory) ESI Mass spectrum: [M+H]+ = 461 Retention time HPLC: 3.2 min (method C).

As the paragraph descriping shows that 5810-56-0 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2008/22979; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

56839-43-1,56839-43-1, 1-(4-Ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(Example 2) Synthesis of salt (ionic liquid) of diclofenac and organic amine compound (1); Synthesis of diclofenac-eperisone salt; Diclofenac sodium (318 mg, 1 mmol) and eperisone hydrochlorate (296 mg, 1 mmol) were dissolved in methanol (5 mL) by heating. The solution was concentrated under reduced pressure, 2-propanol was added to the residue, and the resulting precipitate was filtered off. The filtrate was concentrated under reduced pressure to give a diclofenac-eperisone salt as a colorless glue-like product. infrared absorption spectrum (chloroform): 1680 cm-1 (carbonyl of eperisone), 1605 cm-1 (COO-, COOH of diclofenac free form was 1965 cm-1)

The synthetic route of 56839-43-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Medrx Co., Ltd.; EP2128123; (2009); 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.10338-57-5,4-(Piperidin-1-yl)benzaldehyde,as a common compound, the synthetic route is as follows.

10338-57-5, General procedure: For the reactions, 4-piperidinone or corresponding ketones (1 mmol) and 2-bromobenzaldehyde or corresponding aldehydes(2.5 mmol) were dissolved in ethanol (10 mL). The mixture wasrefluxed at 78 C and added with 0.5 mL 40% NaOH or AcOH/HCl.Reactions were monitored by TLC, when the reactions were accomplished, cooled on ice. The products could precipitate or be purified by crystallization and column chromatography using PE/EA as the eluent. Among these compounds, A4, A6, C5, D1, D2, D3 and D4 were unreported.

10338-57-5 4-(Piperidin-1-yl)benzaldehyde 291354, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Jin, Rong; Chen, Qiuxiang; Yao, Song; Bai, Encheng; Fu, Weitao; Wang, Ledan; Wang, Jiabing; Du, Xiaojing; Wei, Tao; Xu, Haineng; Jiang, Chengxi; Qiu, Peihong; Wu, Jianzhang; Li, Wulan; Liang, Guang; European Journal of Medicinal Chemistry; vol. 144; (2018); p. 218 – 228;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1062580-52-2,(3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride,as a common compound, the synthetic route is as follows.

500 mg of (3R,4R)-1-benzyl-N,4-dimethylpiperidine-3-amine dihydrochloride was added to a 25-mL round-bottomed flask, and 5.00 mL of deionized water was added thereto. After 277 mg of 6-chloro-7-deazapurine and 1.08 of potassium carbonate (K2CO3) were added into the reaction mixture, the reaction mixture was refluxed for about 24 hours and then cooled at room temperature. The reaction mixture was extracted three times with 10.0 mL of dichloromethane (CH2Cl2) to collect an organic phase. The collected organic phase was concentrated under reduced pressure. The resulting residue was purified by flash column chromatography (MeOH:CH2Cl2=2:98). As a result, 282 mg of N-((3R,4R)-1-benzyl-4-methylpiperidine-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-amine was obtained with a yield of about 48.9%. (0285) 282 mg of N-((3R,4R)-1-benzyl-4-methylpiperidine-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-amine was added to a 25-mL round-bottomed flask, and then dissolved with 3.00 mL of methanol. After 280 mg of a 10w/w% palladium/ carbon (Pd/C) was added thereto, a hydrogen-containing balloon was installed on the reaction flask. The reaction mixture was vigorously stirred for about 24 hours and then filtered through a Celite 545 filter agent. The resulting filtrate was concentrated under reduced pressure. The resulting fraction was concentrated under reduced pressure and then further under vacuum. As a result, 200 mg of N-methyl-N-((3R,4R)-4-methylpiperidine-3-yl)-7H-pyrrolo[2,3-d]pyrimidine-4-amine was obtained with a yield of about 97.1%. (0286) 70.0 mg of N-methyl-N-((3R,4R)-4-methylpiperidine-3-yl)-7H-pyrrolo[2,3-d]pyrimidine-4-amine was added to a 5-mL round-bottomed flask, and then dissolved with 1.50 mL of dichloromethane (CH2Cl2). After 57.0 mg of 3-cyanobenzenesulfonyl chloride was added into the solution, the reaction mixture was treated with 0.0750 mL of N,N-diisopropylethylamine and then stirred overnight at room temperature. The reaction mixture was concentrated under reduced pressure, and then the resulting residue was purified by flash column chromatography (MeOH:CH2Cl2=2:98). The resulting fraction was concentrated under reduced pressure and then further under vacuum. As a result, 85.9 mg of 3-(((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)piperidine-1-yl)sulfonyl)benzonitrile was obtained with a yield of about 73.4%. (0287) 1H NMR (400 MHz, CDCl3) delta10.40 (s, 1H), 8.27 (s, 1H), 8.09-8.08 (m, 1H), 8.03-8.01 (m, 1H), 7.95-7.92 (m, 1H), 7.64 (t, J = 3.6 Hz, 1H), 7.13 (d, J = 3.6 Hz, 1H), 6.66 (d, J = 3.6 Hz, 1H), 5.49 (d, J = 4.8 Hz, 1H), 3.79 (dd, J = 4.4, 12.4 Hz, 1H), 3.68 (s, 3H), 3.10 (dd, J = 4.4, 12.4 Hz, 1H), 2.83-2.77 (m, 1H), 2.20-2.11 (m, 1H), 1.92-1.86 (m, 3H), 0.98 (d, J = 6.8 Hz, 3H). (0288) LRMS (ESI) calcd for (C20H22N6O2S + H+) 411.2, found 411.1., 1062580-52-2

As the paragraph descriping shows that 1062580-52-2 is playing an increasingly important role.

Reference：
Patent; Yangji Chemical Co., Ltd.; Han Wha Pharma Co., Ltd.; CHOUGH, Chieyeon; LEE, Sunmin; JOUNG, Misuk; JEONG, Hyun Uk; MOON, Hong-sik; (62 pag.)EP3327021; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

24.64 mg of 4 (0.087 mmol), 41.05 mg of sodium 2-ethyl-hexanoate (0.247 mmol), 20.16 mg of 15 (which may be prepared according to the procedures described in WO 2002/081480, and the content of which is incorporated herein by reference) (0.134 mmol) and 2 ml of THF are successively introduced into a 20 ml round-bottomed flask with stirring and under an argon atmosphere. Stirring is continued for 4 days at r.t. 20 ml of EtOAc are added to the reaction medium, which is then washed successively with 20 ml of NaOH solution (0.1 N), 20 ml of water and 20 ml of saturated NaCl solution. As product has visibly dissolved in the aqueous phase, this aqueous phase is extracted twice with a mixture of 50 ml of CH2Cl2 and 5 ml of MeOH. The 3 organic phases are combined, dried, filtered and then evaporated to dryness. The crude product is purified by PCC with a 93/7 CH2Cl2/MeOH mixture. 28.49 mg of product 16 are collected (Yld=83percent). TLC (90/10 CH2Cl2/MeOH): Rf=0.28 1H NMR (400 MHz, CDCl3): delta (ppm)=7.11 (d, 1H); 5.70 (d, 1H); 5.67 (m, 1H); 5.48 (dd, 1H); 4.72 (m, 1H); 4.20 (d, 1H); 4.02 (d, 1H); 3.80 (d, 1H); 3.50 (s, 1H); 3.49 (s, 3H); 3.36 (m, 2H); 2.54 (m, 2H); 1.96 (m, 2H); 1.47 (s, 6H); 1.02 (s, 9H) LCMS (ES+, 30 V): tR=2.92 mn|m/z=797+ (2M+H+); 399+ (M+H+); 341+ (M+H+[(H3C)2CO]); 841 (2 MH+HCOOH); 443 (MH+HCOOH), 138377-80-7

138377-80-7 3-Aminopiperidin-2-one hydrochloride 19795138, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; AVENTIS PHARMA S.A.; US2007/244087; (2007); 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.162166-99-6,1-Boc-3-Methanesulfonyloxymethyl-piperidine,as a common compound, the synthetic route is as follows.

Raw material 8 (1.0 eq) was added to the reaction flask, and a sufficient amount of ACE was added as a solvent. The mixture was stirred at room temperature, and LiBr (3.0 eq) was slowly added thereto, and the temperature was gradually raised to reflux, overnight. The reaction solution was cooled to room temperature, and the reaction mixture was quenched with water. The reaction mixture was evaporated to dryness, and then the mixture was evaporated and evaporated with EtOAc and water, and the oil layer was collected, and the oil layer was washed three times with saturated brine, and the oil layer was dried over Na 2 SO 4 Product 9, no purification required., 162166-99-6

The synthetic route of 162166-99-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Guangdong Zhongsheng Pharmaceutical Co., Ltd.; Chen Lijuan; Long Chaofeng; Chen Xiaoxin; Liu Zhuowei; Qian Zhiyong; Yang Jinliang; Xiang Mingli; (99 pag.)CN109970740; (2019); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

62718-31-4,62718-31-4, 1-Benzylpiperidine-4-carbonitrile is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step a: To a solution of N^V-diisopropylamine (14.0 mL, 97.5 mmol) in THF (100 mL) was added (at -78 C and under N2) -butyllithium (1.6 M in hexane; 59.0 mL, 94.25 mmol) dropwise. The resulting mixture was stirred for 30 min at RT. 1-benzyl piperidine-4- carbonitrile (6.5 g, 32.5 mmol) in THF (50 mL) was added at -78 C. After stirring for 30 min at this temperature, -propyl iodide (20.5 mL, 211.3 mmol) was added. The resulting mixture was stirred at -78 C for 1 h. The mixture was quenched by addition of saturated aqueous ammonium chloride solution and it was extracted with EtOAc. The combined organic phases were washed with brine, dried over Na2S04, filtered and concentrated to obtain 1 -benzyl -4-propylpiperidine-4- carbonitrile (6.0 g, 24.8 mmol). This compound was used without further purification. MS m/z

The synthetic route of 62718-31-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; CHEN, Christine Hiu-tung; CHEN, Zhuoliang; FORTANET, Jorge Garcia; GRUNENFELDER, Denise; KARKI, Rajesh; KATO, Mitsunori; LAMARCHE, Matthew J.; PEREZ, Lawrence Blas; STAMS, Travis Matthew; WILLIAMS, Sarah; WO2015/107493; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem