Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.73579-08-5,1-Methyl-4-(methylamino)piperidine,as a common compound, the synthetic route is as follows.

To E10 (1.04 g, 3.2 mmol) dissolved in THF (40 mL) was added a solution ofN-methyl-4- (methyl-amino)-piperidine (0.5 mL, 3.2 mmol) in THF (2 mL) followed by addition of NaOH (1.3 mL, 2.5 N, 3.2 mmol) and 3.5 mL of water. The reaction mixture stirred and heated at reflux for 2 hours. The reaction mixture was extracted 3 times using dichloromethane ; the combined organic layers were washed with brine and dried over potassium carbonate. The sample was filtered, concentrated, and the resulting solid was dried overnight under vacuum. Column chromatography (90: 9: 1 v: v: v dichloromethane: methanol: ammonium hydroxide) yielded a light yellow solid (Ell) (164 mg,13percent) ; mp94 C ; HPLC : Inertsil ODS 3VC18, 40 : 30: 30[KH2PO4 (0.01 M, pH 3.2) :CH30H : CH3CN], 264 nm, Rt 3.2 min, 96.7percent purity; MS (TOF ES+) m/z 402.1(M+H, 100),231(41. 5), 202.1 (6)., 73579-08-5

As the paragraph descriping shows that 73579-08-5 is playing an increasingly important role.

Reference£º
Patent; REDDY US THERAPEUTICS, INC.; WO2004/26844; (2004); A1;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.79099-07-3,1-Boc-4-Piperidone,as a common compound, the synthetic route is as follows.

79099-07-3, Trimethylsulfoxonium iodide (13.3 grams, 0.06 mole) was added to a stirred solution of sodium hydride (60 % dispersion in oil, 3.0 grams, 0.126 mole) in THF (150 mL) at 10 C. Reaction mass temperature was slowly raised to RT and stirred further for 2 hours at the same temperature. Reaction mass, was then cooled to 10 C and added M-boc-piperidine-4-one (10 grams, 0.05 mole) solution in THF (50 mL) at the same temperature. Then reaction mass temperature was slowly raised to RT and stirred for 3 hours at same temperature. The progress of the reaction was monitored by. TLC. After completion of the reaction (TLC), the mass was quenched in chilled water (300 mL), the compound was extracted with dichloromethane (3 x 150 mL). The combined organic phase was washed with water (100 mL), brine solution (100 mL) and dried over sodium sulphate. The organic phase was concentrated on rotavacuum to obtain the crude residue, which was further purified by flash chromatography using ethyl acetate: n-hexane ( 15:85) to afford the title compound. Yield: 7.1 grams (66 %). – N R (6 ppm): 1.47 (9H, s), 1.59 – 1.62 (2H. m), 1.76 – 1.83 (2H, m).2.69 (2H, s), 3.39 – 3.45 (2H,m), 3.70 -3.73 (2H, m); Mass(m/z): 158.2 (M-56)+.

79099-07-3 1-Boc-4-Piperidone 735900, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SUVEN LIFE SCIENCES LIMITED; NIROGI, Ramakrishna; SHINDE, Anil Karbhari; JASTI, Venkateswarlu; WO2014/147636; (2014); A1;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4897-50-1,4-Piperidinopiperidine,as a common compound, the synthetic route is as follows.

General procedure: 2-(7-Aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HATU; 1.2 equivalents) was added to a solution of the corresponding alpha-methyl carboxylic acid (2) (1 equiv), the appropriate amine (1.5 equiv) and DIEA (2 equiv) in dry acetonitrile (10 mL) at room temperature under argon atmosphere. The reaction mixture was stirred at room temperature overnight. Solvent was evaporated under reduced pressure, and the crude product was purified using a Teledyne Isco Combiflash? Rf purification machine using 0-10percent CHCl3/methanol as eluent to provide the desired amides 3-59 in 68-95percent yields., 4897-50-1

As the paragraph descriping shows that 4897-50-1 is playing an increasingly important role.

Reference£º
Article; Mathew, Bini; Snowden, Timothy S.; Connelly, Michele C.; Guy, R. Kiplin; Reynolds, Robert C.; Bioorganic and Medicinal Chemistry Letters; vol. 28; 12; (2018); p. 2136 – 2142;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13625-39-3,1,3,8-Triazaspiro[4.5]decane-2,4-dione,as a common compound, the synthetic route is as follows.

13625-39-3, To a suspension of l ,3,8~triazaspiro[4.5]decane-2,4-dione (CAS 13625-39-3, 20 mg, 1 18 mhio, eq. 1) and DIPEA (45.8 mg, 61.9 m, 355 pmol, eq. 3) in AVV-dimethylformamide (0.5 ml) was added 2-chlorobenzo[d]thiazole (22.1 mg, 130 mtho, eq 1.1) The reaction mixture was stirred at 120 C for 2 hours. The reaction mixture was poured into a mixture of ethylacetate/tetrahydrofuran (1 : 1) and the organic layer was washed with water and brine, dried over NazSCri and concentrated in vacuo. The crude material was purified by flash column chromatography (silica gel, eluent: 0 to 5% of methanol in dichloromethane) to afford 8- (benzo[d]thi azol-2-yl)- 1 ,3 , 8-tri azaspiro[4.5]decane-2,4-di one (11 mg, 36.4 mtho, 30.8 %) as a white solid. MS (ISP): 303.1 {I M 1 1 | }.

13625-39-3 1,3,8-Triazaspiro[4.5]decane-2,4-dione 120989, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; C4 THERAPEUTICS, INC.; NASVESCHUK, Christopher, G.; DEY, Fabian; GOERGLER, Annick; KUHN, Bernd; NORCROSS, Roger; ROEVER, Stephan; SCHMID, Philipp; (270 pag.)WO2019/204354; (2019); A1;,
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4897-50-1,4897-50-1, 4-Piperidinopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 101: 2-{[(5E)-2-(l,2-diazinan-l-yl)-4-oxo-4,5-dihydro-l,3-thiazol-5- ylidene]methyl}-5-fluorophenyl 4-(piperidin-l-yl)piperidine-l-carboxylate dihydrochloride; To a solution of 4-piperidinepiperidine (2.O g, 11.9 mmol) in anhydrous CH2Cl2 (50 mL) at 0 0C was added a triphosgene solution (1.3 g, 4.3 mmol) in anhydrous CH2Cl2 (10 mL)by syringe pump addition (1 hour). The mixture was stirred at room temperature overnight. The solid material was removed by filtration. The mixture was extracted with 10% NaHCO3 (2 x 50 mL) and brine (1 x 50 mL). The organic phase was dried over MgSO4, filtered, evaporated, and dried in vacuo, affording the 4-piperidinopiperidinecarbonyl chloride (1.6 g, 59%). The product was used without further purification.To a mixture of (5Z)-2-(l,2-diazinan-l-yl)-5-[(4-fluoro-2-hydroxyphenyl)methylidene]- 4,5-dihydro-l,3-thiazol-4-one (1.0 g, 3.3 mmol) in anhydrous acetonitrile (15 mL) was added potassium carbonate (900 mg, 6.6 mmol), followed by a solution of 4- piperidinopiperidinecarbonyl chloride (1.07 g, 4.6 mmol) in anhydrous acetonitrile (5 mL). The reaction mixture was stirred at reflux for 60 hours. After cooling the mixture to room temperature, the solid material was removed by filtration. The filtrate was recovered and evaporated under reduced pressure. The crude product was purified by flash chromatography (Combiflash Rf, 0-20% MeOH/CH2Cl2). The residue was triturated with diethyl ether (50 mL x 2). The solid material was recovered by filtration and dried in vacuo, affording 2-{[(5E)-2-(l,2- diazinan-l-yl)-4-oxo-4,5-dihydro-l,3-thiazol-5-ylidene]methyl}-5-fluorophenyl 4-(piperidin-l- yl)piperidine-l-carboxylate (954 mg, 57%).To a mixture of 2-{[(5E)-2-(l,2-diazinan-l-yl)-4-oxo-4,5-dihydro-l,3-thiazol-5- ylidene]methyl}-5-fluorophenyl 4-(piperidin-l-yl)piperidine-l-carboxylate (954 mg, 1.9 mmol) in methanol (5 mL) was added a solution of 4M HCl/ dioxane (3 mL, 12.0 mmol). The resultant solution was filtered, and the filtrate was recovered and evaporated. The solid was triturated with diethyl ether (50 mL). The solid material was recovered by filtration and dried in vacuo, affording the final compound (931mg, 91%). 1H NMR (400 MHz, DMSO-J6) 1-45 (m, IH), 1.81 (m, HH), 2.16 (m, 2H), 2.96 (m, 5H), 3.15 (m, IH), 3.44 (m, 3H), 3.88 (m, 2H), 4.11 (m, IH), 4.35 (m,lH) 6.17 (t, IH, J= 6.7 Hz), 7.32 (m, 2H), 7.47 (s, IH), 7.67 (t, IH, J= 6.3 Hz); M+ 502. HPLC purity: 99.1%.

The synthetic route of 4897-50-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHLORION PHARMA, INC.; WO2009/97695; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

7149-42-0,7149-42-0, (1-Methylpiperidin-4-yl)methanamine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The mixture of N-((4-chloro-3-nitrophenyl)sulfonyl)-4-(4-((4′-chloro-5,5-dimethyl- 3,4,5,6-tetrahydro-[l, l’-biphenyl]-2-yl)methyl)piperazin- l-yl)-2-(5-((2- (trimethylsilyl)ethoxy)methyl)pyrazolo[4,3-b]pyrrolo[3,2-e]pyridin- l(5H)-yl)benzamide (200.00 mg, 211.86 mupiiotaomicron, 1.00 eq) and (l-methyl-4-piperidyl)methanamine (81.49 mg, 635.58 //mol, 3.00 eq) were dissolved in CH3CN (10.00 mL), to which DIEA (82.14 mg, 635.58 mupinuomicronChi, 111.00 /L, 3.00 eq) was added in one portion. The resulting mixture was taken up into a microwave tube and heated at 80 C under N2 atmosphere for 2 h. The reacting solution was poured onto silica gel chromatography and eluted with pure DCM to (0281) DCM:MeOH = 5: 1 to afford crude 4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[l, l’- biphenyl]-2-yl)methyl)piperazin- l-yl)-N-((4-(((l-methylpiperidin-4-yl)methyl)amino)-3- nitrophenyl)sulfonyl)-2-(5-((2-(trimethylsilyl)ethoxy)methyl)pyrazolo[4,3-b]pyrrolo[3,2- e]pyridin- l(5H)-yl)benzamide (50.00 mg, 48.27 mupiiotaomicron, 22.79% yield) as a yellow oil which was confirmed by LC-MS.

The synthetic route of 7149-42-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NEWAVE PHARMACEUTICAL INC.; CHEN, Yi; (94 pag.)WO2017/132474; (2017); A1;,
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138007-24-6, tert-Butyl piperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 22: tert-Butyl l-(2-(2,4-dioxo-3,4-dihvdrobenzo[g1pteridin-10(2H)-vI)ethyl)piperidine-4- carboxylate; Step 1 Preparation of tert-butyl l-(cvanomethyl)piperidine-4-carboxylate; [0111] To a solution of tert-butyl piperidine-4-carboxylate (750 mg, 4.05 mmol) in anhydrous DCM (15 mL), is added 2-chloroacetonitrile (333 muL, 5.26 mmol) and potassium carbonate (1.7 g, 12.15 mmol). The reaction mixture is stirred at room temperature for 18 h. The reaction mixture is diluted with water (100 mL) and the aqueous layer is extracted with DCM (100 mL). The organic layer is dried over Na2SO4, filtered, and concentrated under reduced pressure. The residue is dry loaded on silica gel and purified by Biotage flash column chromatography using a gradient from 0 to 10percent MeOH in DCM as eluent. Desired product (463 mg) is isolated (yield: 51 percent). percent). 1H NMR (400 MHz, CDCl3) delta 1.44 (s, 9H), 1.73 (m, 2H), 1.93 (m, 2H), 2.19 (m, 1H), 2.35 (m, 2H), 2.79 (m, 2H), 3.5 l (s, 2H)., 138007-24-6

138007-24-6 tert-Butyl piperidine-4-carboxylate 1512676, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; BIORELIX, INC.; COISH, Philip, D.G.; WICKENS, Philp; AVOLA, Stephanie; BABOULAS, Nick; BELLO, Angelica; BERMAN, Judd; KAUR, Harpreet; MOON, David; PHAM, Vinh; ROUGHTON, Andrew; WILSON, Jeffrey; ARISTOFF, Paul, Adrian; BLOUNT, Kenneth, F.; DIXON, Brian, R.; MYUNG, Jayhyuk; OSTERMAN, David; BELLIOTTI, Thomas, R.; CHRUSCIEL, Robert, A.; EVANS, Bruce, R.; LEIBY, Jeffrey, A.; SCHOSTAREZ, Heinrich, J.; UNDERWOOD, Dennis; NAVIA, Manuel; SCIAVOLINO, Frank; WO2011/8247; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1201935-36-5, 1-(1-Methylpiperidin-4-yl)-1H-pyrazol-4-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0483j To a solution of N-(2-(2-chloropyrimidin-4-yl)-6,7,8 ,9-tetrahydro-5H- benzo [7] annulen-5 -yl)-3 -isopropoxyazetidine- 1 -carboxamide (130 mg, 0.32 mmol) in 1,4- dioxane (5 mL) were added 1-ethyl-1H-pyrazol-4-amine (36 mg, 0.32 mmol), Pd2(dba)3 (29 mg, 0.032 mmol), S-Phos (26 mg, 0.064 mmol) and Cs2CO3 (312 mg, 0.96 mmol). The mixture was stirred at 100 C for 2 h. After diluted with water (50 mL), the mixture was extracted with EtOAc (60 mL x 2). The combined organic layers were dried (Na2SO4), filtered and concentrated. The crude product was purified by prep-HPLC (CH3CN/H20 with 0.05% NH4OH as mobile phase) to give N-(2-(2-(( 1-ethyl-i H-pyrazol-4-yl)amino)pyrimidin-4-yl)-6,7,8 ,9-tetrahydro-5H- benzo[7]annulen-5-yl)-3-isopropoxyazetidine-1-carboxamide as a yellow solid (129 mg, yield:73%). [0499j Synthesis of 3 -(tert-butoxy)-N-(2-(2-(( 1 -(1 -methylpiperidin-4-yl)- 1H-pyrazol-4- yl)amino)pyrimidin-4-yl)-6,7, 8 ,9-tetrahydro-5H-benzo [7] annulen-5 -yl)azetidine- 1 -carboxamide was similar to that of Example 161. The residue was purified by prep-TLC (DCM/MeOH=10/1) to give 3-Qert-butoxy)-N-(2-(2-((1 -(1 -methylpiperidin-4-yl)- 1H-pyrazol-4-yl)amino)pyrimidin- 4-yl)-6,7, 8 ,9-tetrahydro-5H-benzo [7]annulen-5 -yl)azetidine- 1 -carboxamide (33 mg, yield: 41%) as a yellow solid. ESI-MS (M+H) : 573.3. ?H NMR (400 MHz, CD3OD) 5: 8.26 (d, J = 5.2 Hz, 1H), 7.97 (s, 1H), 7.53 (d, J = 7.6 Hz, 1H), 7.77 (s, 1H), 7.57 (s, 1H), 7.26 (d, J = 8.0 Hz, 1H),7.07 (d, J = 5.2 Hz, 1H), 4.94 (d, J = 10.0 Hz, 1H), 4.52-4.46 (m, 1H), 4.15-4.00 (m, 3H), 3.77-3.69 (m, 2H), 2.94-2.79 (m, 4H), 2.23 (s, 3H), 2.17-2.11 (m, 2H), 2.06-1.85 (m, 7H), 1.82-1.72 (m, 1H), 1.61-1.52(m, 1H), 1.30-1.24(m, 1H), 1.11 (s,9H).

1201935-36-5, The synthetic route of 1201935-36-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian, T.; MA, Bin; CHAN, Timothy, Raymond; SUN, Lihong; ZHANG, Lei; KUMARAVEL, Gnanasambandam; LYSSIKATOS, Joseph, P.; KOCH, Kevin; MIAO, Hua; WO2015/89337; (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.3040-44-6,1-(2-Hydroxyethyl)piperidine,as a common compound, the synthetic route is as follows.

A mixture of 20 mg of 2-(4-bromophenyl)-l,3-benzoxazole-5-carbonitrile (INTERMEDIATE 7), 17 mg of 2-piperidin-l-ylethanol, and 8 mg of sodium hydride (60% dispersion in oil) in 1 mL of toluene was purged and flushed with argon. Tris(dibenzylideneacetone) dipalladium (3 mg) and racemic BINAP (3 mg) were added and the mixture was heated to 800C and stirred overnight at this temperature. The reaction mixture was cooled and added directly to a 1000-muM thin-layer chromatography plate, eluting with 4% isopropanol in CH2Cl2 to provide 3.4 mg (15%) of the title compound. Mass spectrum (ESI)348.3 (M+l). 1H NMR (500 MHz, CDCl3): delta 8.18 (d, J=8.5 Hz, 2H), 8.02 (s, IH), 7.63 (m, 2H), 7.05 (d,J=9 Hz, 2H), 4.26 (t, J=6 Hz, 2H), 3.48 (d, J=3Hz, IH), 2.88 (br t, J=5.5 Hz, 2H), 2.61 (m, 3H), 1.68 (m, 5H), 1.49 (m, IH)., 3040-44-6

As the paragraph descriping shows that 3040-44-6 is playing an increasingly important role.

Reference£º
Patent; MERCK & CO., INC.; WO2007/70173; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

21987-29-1, 4,4-Difluoropiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 100 mL flask was placed 4-[5-(2-tert-butyl-4-pyridyl)-3-thienyl]-3-chloro-benzoic acid (150 mg, 0.40 mmol, 1 eq.) in DMF (10 mL), followed by addition of DIPEA (0.37 mL, 1.61 mmol, 5 eq.) and HATU (307 mg, 0.80 mmol, 2 equiv), and the resulting mixture was stirred for 5 min at RT and 3,3-difluoropiperidine (196 mg, 1.61 mmol, 4 eq.) were added and the mixture stirred at RT under nitrogen atmosphere overnight. The progress of the reaction was monitored by TLC and LCMS. After completion of reaction, the mixture was diluted with water (100 mL) and extracted with EtOAc (2*100 mL), washed with water (4*100 mL) then dried over anhydrous sodium sulfate and the combined organic layer was concentrated under reduced pressure to give a viscous compound, which was purified by reverse phase HPLC process to afford [4-[5-(2-tert-butyl-4-pyridyl)-3-thienyl]-3-chloro-phenyl]-(4,4-difluoro-1-piperidyl) methanone (50 mg) as an off-white solid, the free base. 1H NMR (400 MHz, Methanol-d4) delta (ppm): 8.49 (d, J=5.2 Hz, 1H), 7.91 (s, 1H), 7.78 (s, 1H), 7.71-7.61 (m, 3H), 7.52 (d, J=5.2 Hz, 1H), 7.47 (d, J=7.9 Hz, 1H), 3.87 (t, 2H), 3.62 (t, 2H), 2.08 (t, 4H), 1.42 (s, 9H). LCMS: (M+1) 475.2.

21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Medivation Technologies LLC; Pujala, Brahmam; Jangir, Ramniwas; Guguloth, Rambabu; Shinde, Bharat Uttam; Rai, Roopa; Pham, Son Minh; Bernales, Sebastian; Lindquist, Jeffrey; Guha, Mausumee; Kallem, Satyanarayana; Bhatt, Bhawana; Bhagwat, Vikas Ramdas; (162 pag.)US2018/51013; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem