Category: piperidines

170737-53-8, Methyl N-Cbz-4-piperidineacetate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B: Benzyl 4-[l-fmethoxycarbonyl)-3-phenylbut-3-en-l-yl]piperidine-l-carboxylate; Lithium hexamethyldisilylazide (1.0 M in THF; 7.31 mL, 7.31 mmol) was added to solution of benzyl 4-(2-methoxy-2-oxoethyl)piperidine-l-carboxylate (1.94 g, 6.65 mmol) in tetrahydrofuran (35 mL) at -78 0C. After 40 min, [l-(bromomethyl)vinyl]benzene (1.08 mL, 7.31 mmol) was added and the reaction mixture was warmed to ambient temperature. After 18 h, the mixture was quenched with saturated aqueous ammonium chloride and extracted with ethyl acetate (2x). The combined organic extracts were dried over magnesium sulfate, filtered and concentrated. Purification by silica gel chromatography (100% hexanes -? 40% hexanes/ ethyl acetate) gave the title compound (2.11 g). MS 408.2 (M+l)., 170737-53-8

170737-53-8 Methyl N-Cbz-4-piperidineacetate 40429392, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK & CO., INC.; WO2006/44504; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

140645-24-5, (S)-3-(Aminomethyl)-1-N-Boc-piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: HATU (1.2 equiv) and DIEA (1.5 equiv) were added to a solutionof 2-fluoro-4-nitrobenzoic acid (1 equiv) and R6-NH2 (1 equiv) inCH2Cl2 at rt. The resulting mixture was heated to 25e40 C andstirred until the reaction was complete. The mixture was dilutedwith ethyl acetate, and the organic layer was washed with saline,dried over anhydrous Na2SO4 and filtered. The filtrate wasconcentrated and purified using chromatography to yield the intermediates33a-g. Intermediates 33a-g (1 equiv) were dissolved inethanol, and Pd/C (0.1 equiv)was added. The flask was flushed withH2 and stirred for 6 h at 40 C. The reaction mixture was filteredthrough a Celite pad and the filtrate was concentrated to dryness,yielding intermediates 34a-g.

140645-24-5, The synthetic route of 140645-24-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Chen, Yixuan; Cheng, Maosheng; Hao, Chenzhou; Wang, Ruifeng; Wu, Tianxiao; Yang, Bowen; Yu, Sijia; Zhao, Dongmei; Zhao, Xiangxin; European Journal of Medicinal Chemistry; vol. 188; (2020);,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.71985-80-3,1-Methylpiperidine-4-carboxylic acid hydrochloride,as a common compound, the synthetic route is as follows.

71985-80-3, Example 8; Synthesis of 2-(benzhvdryl(methylamino)-l-(4-((l-methylpiperidin-4- yl)(phenyl)methyl)piperazin-l-yl)ethanone (compound no. 14); A. Synthesis of (l-methylpiperidin-4-yl)(phenyl)methanone[0096] l-Methylpiperidine-4-carboxylic acid hydrochloride salt 10 g (55.7mmol) was added to thionyl chloride (25 ml) and stirred at room temperature until the solid dissolved completely. The reaction mixture was stirred for another 20 minutes and concentrated. The product was used for the next step without further purification.[0097] To a cooled suspension of anhydrous aluminum chloride (20 g, 75 mmol) in benzene 30 ml at 00C was added l-methylpiperidine-4-carboxylic acid chloride in small portions and the resulting mixture was refluxed for 3 hours. The reaction mixture was then cooled down by adding to ice water. The organic phase was discarded. The aqueous solution was washed with 2×50 ml ethyl ether, basified with potassium hydroxide pellet slowly to pH >10 and extracted with ethyl ether 4×50 ml. The combined ethereal solution was dried over sodium sulfate and concentrated to give 9.5 g of desired product in 84% yield.

The synthetic route of 71985-80-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NEUROMED PHARMACEUTICALS LTD.; WO2007/71035; (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.62718-31-4,1-Benzylpiperidine-4-carbonitrile,as a common compound, the synthetic route is as follows.

Example VI To 7 parts of magnesium is added dropwise a solution of 50 parts of 1-bromo-2-methylbenzene in 140 parts of 1,1′-oxybisethane so that the mixture is refluxing. The whole is stirred for 15 minutes at reflux. The Grignard-complex is cooled to 10 C. and there is added dropwise a solution of 30 parts of 1-(phenylmethyl)-4-piperidinecarbonitrile in 70 parts of 1,1′-oxybisethane. Upon completion, stirring is continued for 4 hours at room temperature. The reaction mixture is decomposed with a solution of 40 parts of ammonium chloride in 400 parts of water. The organic phase is separated, dried, filtered and evaporated, yielding 31 parts of (2-methylphenyl) [1-(phenylmethyl)-4-piperidinyl]methanone as an oily residue. In a similar manner there is also prepared: (4-fluorophenyl) [4-methyl-1-(phenylmethyl)-4-piperidinyl]methanone as an oily residue., 62718-31-4

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

Reference：
Patent; Janssen Pharmaceutica N.V.; US4342870; (1982); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

61869-08-7, (3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,61869-08-7

0.8 g of oily paroxetine free base and 1.13 g of glycocholic acid were completely dissolved in 20 mL of ethanol while heating to 40 C. with shaking for 3 hours. After the solution was concentrated under reduced pressure until about 5 mL of the solvent was left, it was allowed to stand at -20 C.0 C. for 24 hours to precipitate a crystal, followed by filtration. The filtered residue was washed with cold methanol at 0 C. or less, and dried under vacuum to give 1.6 g of solid paroxetine glycocholate as a light gray powder.

61869-08-7 (3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine 44274603, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Lee, Sang Joon; Shin, Hee Jong; Ki, Min Hyo; Lee, Su Kyoung; Kim, Bok Young; Lee, Hong Woo; US2006/63747; (2006); 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.109384-19-2,tert-Butyl 4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of N-Boc-4-hydroxypiperidine (600 mg, 3.0 mmol) in HCl/Et20 (2.0 M, 10 mL) was stirred at room temperature for 2 hours. The reaction mixture was concentrated and the residue obtained washed with Et20 and dried to give the title product (370 mg, 90percent) as white solid which was used without purification.

109384-19-2, 109384-19-2 tert-Butyl 4-hydroxypiperidine-1-carboxylate 643502, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; CTXT PTY LIMITED; BERGMAN, Ylva Elisabet; CAMERINO, Michelle Ang; STUPPLE, Paul Anthony; (81 pag.)WO2017/153520; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

149554-03-0, tert-Butyl 2-(4-oxopiperidin-1-yl)acetate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example A13e a) Preparation of Int. 229 3-Nitro-aniline (5.0 g; 36.2 mmol) was dissolved in DCE (75 ml). Tert-butyl 4- oxopiperidine-1 -acetate (15.4 g; 72.4 mmol) and acetic acid (4.3 g; 72.4 mmol) were added. The mixture was stirred at r.t. for 1 h, then sodiumacetoxyboro hydride (15.3 g; 72.4 mmol) was added in portions. The mixture was stirred at r.t. overnight. The mixture was washed with water, brine, dried, and concentrated to give 3.0 g of Int. 229 (69.5 %).

149554-03-0, The synthetic route of 149554-03-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; JANSSEN PHARMACEUTICA NV; DIELS, Gaston, Stanislas, Marcella; SCHOENTJES, Bruno; VERSELE, Matthias, Luc, Aime; BERTHELOT, Didier, Jean-Claude; WILLEMS, Marc; VIELLEVOYE, Marcel; SOMMEN, Francois, Maria; WROBLOWSKI, Berthold; MEERPOEL, Lieven; WO2015/150557; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 44: tert-butyl 1-oxo-2,7-diazaspiro[4,5]decane-7-carboxylate (P44)2,7-diazaspiro[4.5]decan-l-one hydrochloride (600 mg, 3.15 mmol), was dissolved in 30 m L of DCM. To this solution, TEA (1.98 mL, 14.18 mmol) and Boc20 (895 mg, 4.10 mmol) were added and the reaction mixture was stirred at RT for 4 hrs. Water was added and the two layers were separated; the organic layer was washed with NH4CI, dried and evaporated to obtain ferf-butyl l-oxo-2,7- diazaspiro[4.5]decane-7-carboxylate (p44, 830 mg, y= quant.), colourless oil.MS (ES) (m/z): 255.2 [M+H]+., 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SHIRE INTERNATIONAL GMBH; SEMERARO, Teresa; TARSI, Luca; MICHELI, Fabrizio; LUKER, Tim; CREMONESI, Susanna; (122 pag.)WO2016/42451; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

72551-53-2, Ethyl 1-benzylpiperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,72551-53-2

A 4N-aqueous sodium hydroxide solution (15 ml) was added to a solution of ethyl 1-benzyl-3-piperidinecarboxylate (7.00 g, 28.3 mmol) in a mixture of tetrahydrofuran (30 ml) and 1,4-dioxane (30 ml), and the resulting mixture was stirred at room temperature for 4 hours. After a 4N-aqueous sodium hydroxide solution (15 ml) was added again, the resulting mixture was stirred overnight at room temperature. After completion of the reaction, the reaction solution was neutralized by the addition of 2N-hydrochloric acid (15 ml) under ice-cooling and the resulting mixture was subjected to azeotropic concentration with toluene. The residue was suspended in ethanol, followed by filtration, and the filtrate was concentrated to obtain 1-benzyl-3-piperidinecarboxylic acid (6.3 g, 100%).

The synthetic route of 72551-53-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Sumitomo Pharmaceuticals Company, Limited; EP1403255; (2004); 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.10315-06-7,Methyl 1-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

To A SOLUTION OF BULI (12. 4 ML OF A 1. 6 M SOLUTION IN HEXANE, 19. 8 MMOL) IN THF (25 mL) COOLED TO-78 C, ACETONITRILE (1 ML) WAS ADDED DROPWISE UNDER ARGON atmosphere. After stirring the resulting suspension for 5 min AT-78 C, A SOLUTION of methyl 1-BENZYLPIPERIDINE-4-CARBOXYLATE (2. 0 G, 8. 1 MMOL, OBTAINED IN THE previous section) IN THF (5 ML) WAS ADDED DROPWISE AND STIRRED FOR 30 min AT-78 C. It was allowed to reach room temperature and stirred at this temperature overnight. 1 N HCI WAS ADDED TO ADJUST THE PH TO 7 and the aqueous phase was extracted with CHCI3. The organic phase was dried over NA2S04 and concentrated to dryness, to afford 1. 92 G OF THE DESIRED COMPOUND IN A SOLID orange form (YIELD : 98%)., 10315-06-7

The synthetic route of 10315-06-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; J. URIACH Y COMPANIA S.A.; WO2004/76450; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem