Day: October 23, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.25519-78-2,(4-Fluorophenyl)(piperidin-4-yl)methanone hydrochloride,as a common compound, the synthetic route is as follows.

25519-78-2, 5-Methyl-3-phenylisooxazole-4-carboxylic acid (40 mg, 0.197 mmol), 4-(4-Fluorobenzoyl)piperidine hydrochloride (31.4 mg, 0.151 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (37.7 mg, 0.197 mmol) and triethylamine (59.8 mg, 0.591 mmol) were mixed in dichloromethane (2 ml) and stirred at room temperature over night. Solvent was evaporated in vacuo, and the residue was taken up in methanol (1 mL), filtered and purified by preparative chromatography. The fractions were partitioned between NaHCO3 (sat) and ethylacetate. The organic layer was washed with water and concentrated in vacuo to afford the title compound. HRMS (ESI, pos. ion) m/z calcd for C23H21FN2O3: 392.1536, found 392.1542.

25519-78-2 (4-Fluorophenyl)(piperidin-4-yl)methanone hydrochloride 3084438, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Amgen Inc.; Biovitrum AB; US2008/21022; (2008); 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.24666-56-6,3-Aminopiperidine-2,6-dione hydrochloride,as a common compound, the synthetic route is as follows.

3-Hydroxyphthalic anhydride (1.641 g, 10 mmol, 1 eq) and 3-aminopiperidine-2,6- dione hydrochloride (1.646 g, 10 mmol, 1 eq) were dissolved in pyridine (40 mL, 0.25 M) and heated to 110 C. After 14 hours, the mixture was cooled to room temperature and concentrated under reduced pressure. Purification by column chromatography (ISCO, 24 g silica column, 0-10% MeOH/DCM) afforded the desired product as a tan solid (2.424 g, 8.84 mmol, 88%)., 24666-56-6

The synthetic route of 24666-56-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; BUCKLEY, Dennis; BRADNER, James; REMILLARD, David Ian; (212 pag.)WO2017/223452; (2017); 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.54012-73-6,Piperidin-3-amine,as a common compound, the synthetic route is as follows.

The steps will be a 2, 3 – diphenyl maleic anhydride (125g) and 3 – amino piperidine (50.1g) mixing, adding 1L dichloromethane, stirring at room temperature for 1 hour, the solvent is removed. Residue by adding acetic anhydride and sodium acetate mixture, heating to reflux 2 hours, after the reaction is complete, cooling, adding water and ethyl acetate extraction, to obtain the compound of formula d (150.5g, yield 90.6%)., 54012-73-6

The synthetic route of 54012-73-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Borui Bio-pharmaceutical (Suzhou) Co., Ltd.; Yuan Jiandong; (12 pag.)CN103450201; (2017); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.137076-22-3,tert-Butyl 4-formylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl 4-formylpiperidine-1-carboxylate (1.00 g, 4.69 mmol) in MeOH (10 mL) was added morpholine (613 mg, 7.04 mmol). The resulting mixture was stirred for 6 hr, then NaBH3CN (444 mg, 7.07 mmol) was added. The resulting solution was stirred at room temperature overnight and quenched with H2O (1 mL). The resulting mixture was concentrated under vacuum. The residue was purified by flash chromatography on silica gel eluting with 3% MeOH in DCM. This resulted in 1.0 g (75%) of tert-butyl 4-(morpholin-4-ylmethyl) piperidine-1-carboxylate as yellow oil. LCMS (Method 25) [M+H]+=285.0, RT=0.59 min., 137076-22-3

The synthetic route of 137076-22-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Genentech, Inc.; Zak, Mark Edward; Ray, Nicholas Charles; Goodacre, Simon Charles; Mendonca, Rohan; Kellar, Terry; Cheng, Yun-Xing; Li, Wei; Yuen, Po-Wai; US2015/336962; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

184637-48-7, tert-Butyl 3-aminopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 6 Intermediate 6.1: 3-tert-Butoxycarbonylamino-1,1-bis-[3-(4-methoxy-phenyl)-propyl]-piperidinium trifluoroacetate Piperidin-3-yl-carbamic acid tert-butyl ester (1 g, 5 mmol) and 1-(3-Bromo-propyl)-4-methoxy-benzene (2.3 ml, 13 mmol), potassium carbonate (1.6 g, 11.6 mmol) and sodium iodide (1.3 g, 8.7 mmol) are dissolved in acetonitril (40 ml) and stirred at reflux for 5 days. The solvent is removed under vacuo and the product purified by preparative HPLC-MS (MeOH/H2O+0.1percent TFA). LC (method F): tR=1.89 min; Mass spectrum (ESI+): m/z=497 [M]+.

184637-48-7, The synthetic route of 184637-48-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WIEDENMAYER, Dieter; HECKEL, Armin; HAMPRECHT, Dieter; US2015/45326; (2015); 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.7149-42-0,(1-Methylpiperidin-4-yl)methanamine,as a common compound, the synthetic route is as follows.

7149-42-0, A solution of the appropriate chloride (1 eq) (ex: 5-chloro-6-methyl-3-(3- trifluoromethoxy-phenyl)-7,8-dihydro-6H-9-oxa-1 ,2,3a,4,6-pentaaza-cyclopenta- (ajnaphthalene) and the appropriate amine (3 to 5 eq) (ex: 1-methyl-piperidin-4- ylamine) in nBuOH (15 mL/mmol) was heated up to 180- 185C under microwave irradiation for 5 h – 10 h (or 24 h at 160-180C in a silicon bath). The solvent was evaporated under vacuum and the residue was purified by flash chromatography (Isolute/Flash, Sill, 2.5% MeOH with 7N ammonia in DCM) or by semi-preparative HPLC (Gemini C18 (150 10 mm; 5 m), Solvent A: water with 0.1 % formic acid; Solvent B: acetonitrile with 0.1 % formic acid. Gradient: 40% of A to 0% of A).The NH-BOC-protected amines got deprotected in the reaction conditions and reacted giving a mixture of regioisomers. Amine: (1-methyl-4-piperidinyl)methylamineHPLC-MS (method 1 ): Rt = 3.28 min, [M+H]+ m/z 492.1. NMR (300 MHz, DMSO-d6) delta 8.58 (s, 1 H), 8.43 (d, J = 7.9 Hz, 1 H), 8.20 (s, 1 H), 7.69 (m, 1 H), 7.49 (m, 1 H), 6.91 (s, 1H), 4.46 (m, 1 H), 3.20 (m, 4H), 2.80 (m, 2H), 2.70 (s, 3H), 2.17 (s, 3H), 1.89 (m, 3H), 1.72 (m, 2H), 1.46 (d, J = 6.2 Hz, 3H), 1.25 (m, 2H).

As the paragraph descriping shows that 7149-42-0 is playing an increasingly important role.

Reference£º
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); GARCIA COLLAZO, Ana Maria; PASTOR FERNANDEZ, Joaquin; BLANCO APARICIO, Carmen; RODRIGUEZ HERGUETA, Antonio; MARTIN HERNANDO, Jose Ignacio; RAMOS LIMA, Francisco Javier; HERNANDEZ HIGUERAS, Ana Isabel; SALUSTE, Carl-Gustave Pierre; GONZALEZ CANTALAPIEDRA, Esther; MARTINEZ GONZALEZ, Sonia; SALGADO SERRANO, Antonio; NOYA MARINO, Beatriz; WO2011/80510; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1037834-62-0, 6-Azaspiro[2.5]octane hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-(chloroacetyl)-6-azaspiro[2.5]octane; Dissolved 6-azoniaspiro[2.5]octane chloride (1.1g, 7.5 mmol) and 2N sodium carbonate (9.3 ml, 19 mmol) in DCM (10 ml) while stirring in an ice bath. Slowly added 2- chloroacetyl chloride (0.712 ml, 9 mmol) dropwise and stirred cold for 30 minutes. The reaction mixture was stirred at room temperature for 1 h, and subsequently was diluted with dichloromethane (DCM, 20 ml) and water (20 ml). Separated layers and extracted aqueous layer twice with DCM. Combined organics were washed with brine, dried over sodium sulfate, filtered, and concentrated to yield pale-yellow oil (1 ,39g, 99%).Experimental Data; LCMS 50% H2O, Retention time 1.916 min., Parent C9Hi4CINO, MW 187.08; Found APCI+ 188.1 (M+1); 1H NMR (CDCI3) delta 4.05 (s, 2H), 3.7-3.4 (m, 4H), 1.50-1.30 (m, 4H), 0.35 (s, 4H)., 1037834-62-0

1037834-62-0 6-Azaspiro[2.5]octane hydrochloride 54593187, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/84300; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

336191-17-4, tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of compound 24 (300.00 mg, 1.25 mmol, 1.00 eq.) and benzoic acid (183.18 mg, 1.50 mmol, 1.20 eq.) in DCM (6 mL) was added NMM (252.88 mg, 2.50 mmol, 2.00 eq.) and T3P (1.19 g, 1.88 mmol, 1.50 eq.). The mixture was stirred at 25 C for 4 hrs.Then the mixture was purified by TLC (PE:EtOAc=1:1) to compound 25 (310.00 mg, 899.99 umol, 72.00% yield). To a solution of compound 25 (310.00 mg, 899.99 umol, 1.00 eq.) in DCM (2 mL) was added HCl/AcOEt (30mL) at 0 C. The mixture was stirred at 25 C for 2 hrs. Then it was concentrated to dryness to give compound 26 (300.00 mg, crude). To a solution of compound 6 (20.00 mg, 66.39 umol, 1.00 eq.) and compound 26 (19.47 mg, 79.67 umol, 1.20 eq.) in pyridine (3.00 mL) was added EDCI (19.09 mg, 99.59 umol, 1.50 eq.) at 25 C , the mixture was stirred for 3 h our at 25 C. LCMS showed the SM consumed, desired product was formed as major product. The reaction was concentrated, dissolved in to DMF (3 mL), purified by prep-HPLC (base condition) and concentrated to give SC27 (11.00 mg, 20.37 umol,30.68% yield, 97.7% purity) as yellow gum.

336191-17-4, As the paragraph descriping shows that 336191-17-4 is playing an increasingly important role.

Reference£º
Article; Tuyishime, Marina; Lawrence, Rae; Cocklin, Simon; Bioorganic and Medicinal Chemistry Letters; vol. 26; 1; (2016); p. 228 – 234;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

3970-68-1, 4-Methylpiperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 5-mL microwave vials, secondary amines (0.164 mmol) (commercially available, known from the literature) and K2CO3 solid (37.7 mg, 0.273 mmol) were added followed by addition of 1 mL DMF solution of the mixture of 3-bromo-N,N-bis(4- methoxybenzyl)-2-(l -(4-methoxybenzyl)- lH-tetrazol-5-yl)-6- (trifluoromethyl)benzenesulfonamide and 3-bromo-N,N-bis(4-methoxybenzyl)-2-(2-(4- methoxybenzyl)-2H-tetrazol-5-yl)-6-(trifluoromethyl)benzenesulfonamide from Reference Example 24 (40 mg, 0.055mmol). The vials were capped and heated at 140C with stirring for 2 hr. After the vials were cooled to room temperature, the solvent was removed in a GeneVac. Into each residue was added 500 of 3 N HC1 and 2 mL of EtOAc. The organic layers were transferred into 2 dram vials. The organic solvent was removed in GeneVac to afford the crude intermediates which were deprotected without further purification in the subsequent step., 3970-68-1

As the paragraph descriping shows that 3970-68-1 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; MANDAL, Mihir; TANG, Haifeng; XIAO, Li; SU, Jing; LI, Guoqing; YANG, Shu-Wei; PAN, Weidong; TANG, Haiqun; DEJESUS, Reynalda; HICKS, Jacqueline; LOMBARDO, Matthew; CHU, Hong; HAGMANN, William; PASTERNAK, Alex; GU, Xin; JIANG, Jinlong; DONG, Shuzhi; DING, Fa-Xiang; LONDON, Clare; BISWAS, Dipshikha; YOUNG, Katherine; HUNTER, David, N.; ZHAO, Zhiqiang; YANG, Dexi; WO2015/112441; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

496807-97-7,496807-97-7, 3,3-Difluoropiperidine hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3,3-difluoropiperidine hydrochloride (518 mg) in DMF (15 mL) was added cesium carbonate (3.21 g) and (3-bromopropoxy)-tert-butyldimethylsilane (0.838 mL). The resulting reaction mixture was heated to 50 C. for 1.5 hours before cooling back to room temperature. Water and ethyl acetate were added to the reaction mixture. The mixture was extracted with ethyl acetate (2¡Á). The combined organics were washed with water (2¡Á), brine, dried over magnesium sulfate, filtered and concentrated. Purification by flash chromatography (ISCO, 0 to 40% ethyl acetate in hexanes with 1% triethylamine) gave the desired product (612 mg). 1H NMR (400 MHz, CDCl3): delta (ppm) 4.20 (t, 1H), 3.71-3.64 (m, 2H), 3.46 (t, 1H), 2.62 (t, 1H), 2.50-2.47 (m, 1H), 2.44-2.42 (m, 1H), 2.05-1.98 (m, 1H), 1.91-1.82 (m, 2H), 1.77-1.67 (m, 4H), 0.89 (d, 9H), 0.05 (s, 3H), 0.04 (s, 3H).

As the paragraph descriping shows that 496807-97-7 is playing an increasingly important role.

Reference£º
Patent; MSD Italia S.R.L.; Merck Sharp & Dohme Corp.; Rudd, Michael T.; McCauley, John; Liverton, Nigel; Grise-Bard, Christiane; Brochu, Marie-Christine; Charron, Sylvie; Aulakh, Virender; Bachand, Benoit; Beaulieu, Patrick; Zaghdane, Helmi; Han, Yongxin; Ferrara, Marco; Harper, Steven; Summa, Vincenzo; Chackalamannil, Samuel; Venkatraman, Srikanth; Shah, Unmesh; Velazquez, Francisco; (211 pag.)US9328138; (2016); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem