Category: 5747-48-8

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5747-48-8

Example I. Synthesis of quetiapine by reductive alkilation of 11-piperazindibenz[b,f][1,4]thioazepine with (2-hydroxyethoxy)acetaldehyde in the presence of sodium borohydride. The mixture of 11-piperazindibenz[b,f][1,4]thioazepine (1 g, 0,0034 mol), sodium acetate (0,8 g, 0,01 mol), glacial acetic acid (4 cm3), (2-hydroxyethoksy)acetaldehyde (0,35g, 0,0034 mol) and water (50 cm3) is cooled to 0C. Next sodium borohydride was slowly (40 min) added (5 g, 0,13 mol) in temperature 0C. After this time the mixture was stirred for 1 h in temperature 10C and 10% aq NaOH was added (to pH about 8-9). The mixture was extracted with diethyl ether (3×30 cm3), organic faze was dried by sodium sulfate. The product (1.17g) was obtain with purity about 98% (HPLC)

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Celon Pharma Sp. z o.o.; EP1602650; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine. 11-Piperazinyldibenzo[b,f][1,4]thiazepine (0.1 mole), sodium carbonate (0.18 mole), sodium iodide (0.016 mole) and 2-chloroethoxyethanol (0.108 mole) were combined together in toluene (250 ml) and N-methylpyrrolidone (55 ml). The reaction was heated at reflux over 24 hours. The reaction was cooled and washed with water (1 x 175 ml., 2 x 60 ml.). The organic phase was dried by azeotropic distillation. A solution of fumaric acid (0.06 mole) in ethanol (110 ml) was added to the toluene solution at 60-70C. On cooling the hemifumarate salt crystallized out and was isolated by filtration in 75% yield, m.pt 172-173C.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; IMPERIAL CHEMICAL INDUSTRIES PLC; EP282236; (1988); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine. 11-Piperazinyldibenzo[b,f][1,4]thiazepine (0.1 mole), sodium carbonate (0.18 mole), sodium iodide (0.016 mole) and 2-chloroethoxyethanol (0.108 mole) were combined together in toluene (250 ml) and N-methylpyrrolidone (55 ml). The reaction was heated at reflux over 24 hours. The reaction was cooled and washed with water (1 x 175 ml., 2 x 60 ml.). The organic phase was dried by azeotropic distillation. A solution of fumaric acid (0.06 mole) in ethanol (110 ml) was added to the toluene solution at 60-70C. On cooling the hemifumarate salt crystallized out and was isolated by filtration in 75% yield, m.pt 172-173C.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; IMPERIAL CHEMICAL INDUSTRIES PLC; EP282236; (1988); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, (E)-2-(4-(dibenzo[b,fJ[l,4]thiazepin-l l-yl)piperazin-l-yl)ethanol-d4 prepared according to general method A in 52 % yield. This material was carried forward in crude form.[126] 1H NMR (CDCl3) delta 2.52 – 2.57 (m, 2H), 2.63 – 2.68 (m, 2H), 3.47 – 3.60 (m, 2H), 3.65 (t, 2H, J= 6.4), 6.89 (t, IH, J= 7.6), 7.07 (d, IH, J= 7.6), 7.15 – 7.19 (m, IH), 7.27 – 7.36 (m, 3H), 7.39 (d, IH, J= 7.6) 7.5 l (d, IH, J= 7.3). LCMS mlz 343.9 [M + H].

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CONCERT PHARMACEUTICALS INC.; WO2008/66620; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 8 1-piperazinyldibenzo[b,f][1,4]thiazepine A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11-chlorodibenzo[b,f][1,4]thiazepine in toluene [52 gm (0.22 moles)], and the mixture was stirred for 15 min 45-50 C. To the resulting solution was added piperazine 73.0 (0.84 moles) at 45-50 C. The reaction mixture was heated to 70-80 C. The reaction mixture was maintained at 70 C. to 80 C. for 120-180 min. The reaction mixture was analyzed by HPLC (to check for absence of compound of formula III) and was cooled to 20 C. to 25 C. The reaction mixture was added 250 cc DM water and was stirred for 30 min. at 25-30 C. The layers were separated and the organic layer washed with 250 cc DM water. The organic phase was distilled off under vacuum below 70 C. Traces of toluene were removed by adding n-butanol. To the resultant oily mass was added 150 cc n-butanol. The mixture was stirred for 24 hrs and chilled to 0-5 C. The reaction mass was filtered with the filtrate (mother liquor) containing 11-piperazinyldibenzo[b,f][1,4]thiazepine. Purity of 11-piperazinyldibenzo[b,f][1,4]thiazepine in toluene was more than 98.0% (area % by HPLC).

5747-48-8, As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; Kansal, Vinod Kumar; Ahmad, Suhail; Lal, Kanhaiya; Patil, Bhatu Tumba; US2008/241949; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, (E)-2-(4-(dibenzo[b,fJ[l,4]thiazepin-l l-yl)piperazin-l-yl)ethanol-d4 prepared according to general method A in 52 % yield. This material was carried forward in crude form.[126] 1H NMR (CDCl3) delta 2.52 – 2.57 (m, 2H), 2.63 – 2.68 (m, 2H), 3.47 – 3.60 (m, 2H), 3.65 (t, 2H, J= 6.4), 6.89 (t, IH, J= 7.6), 7.07 (d, IH, J= 7.6), 7.15 – 7.19 (m, IH), 7.27 – 7.36 (m, 3H), 7.39 (d, IH, J= 7.6) 7.5 l (d, IH, J= 7.3). LCMS mlz 343.9 [M + H].

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CONCERT PHARMACEUTICALS INC.; WO2008/66620; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 8 1-piperazinyldibenzo[b,f][1,4]thiazepine A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11-chlorodibenzo[b,f][1,4]thiazepine in toluene [52 gm (0.22 moles)], and the mixture was stirred for 15 min 45-50 C. To the resulting solution was added piperazine 73.0 (0.84 moles) at 45-50 C. The reaction mixture was heated to 70-80 C. The reaction mixture was maintained at 70 C. to 80 C. for 120-180 min. The reaction mixture was analyzed by HPLC (to check for absence of compound of formula III) and was cooled to 20 C. to 25 C. The reaction mixture was added 250 cc DM water and was stirred for 30 min. at 25-30 C. The layers were separated and the organic layer washed with 250 cc DM water. The organic phase was distilled off under vacuum below 70 C. Traces of toluene were removed by adding n-butanol. To the resultant oily mass was added 150 cc n-butanol. The mixture was stirred for 24 hrs and chilled to 0-5 C. The reaction mass was filtered with the filtrate (mother liquor) containing 11-piperazinyldibenzo[b,f][1,4]thiazepine. Purity of 11-piperazinyldibenzo[b,f][1,4]thiazepine in toluene was more than 98.0% (area % by HPLC).

5747-48-8, As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; Kansal, Vinod Kumar; Ahmad, Suhail; Lal, Kanhaiya; Patil, Bhatu Tumba; US2008/241949; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics