Category: 61869-08-7

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in 10 mL of dimethylsulfoxide with stirring for 5 minutes. The solution was slowly added dropwise to 100 mL of purified water to precipitate a solid, stirred at 0 C. for 3 hours, and filtered. The filtered residue was washed with 30 mL of ethyl ether, and dried under vacuum to give 1.7 g of solid paroxetine cholate as a white powder., 61869-08-7

As the paragraph descriping shows that 61869-08-7 is playing an increasingly important role.

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

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.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.,61869-08-7

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were suspended in 50 mL of isopropanol. After the suspension was refluxed with stirring for 3 hours, it was slowly stirred at 25 C. for 2 hours, filtered and followed by drying under vacuum, yielding 2.15 g of solid paroxetine cholate as a white crystal.

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

61869-08-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in 20 mL of methanol while heating to 40 C. with shaking for 2 hours. The solvent was removed under reduced pressure, and then the residue was dried under vacuum, yielding 2.2 g of solid paroxetine cholate as a white powder. ; EXAMPLE 3 1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in 10 mL of methanol while heating to 40 C. with shaking for one hour. The solution was slowly added dropwise to 100 mL of ethyl ether to precipitate a solid, stirred at 0 C. for 3 hours, and filtered. The filtered residue was washed with 30 mL of ethyl ether, and dried under vacuum to yield 1.89 g of solid paroxetine cholate as a light gray powder.

As the paragraph descriping shows that 61869-08-7 is playing an increasingly important role.

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

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

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in 10 mL of N,N-dimethylformamide with stirring for 10 minutes. The solution was slowly added dropwise to 100 mL of isopropyl acetate to precipitate a solid, stirred at 0 C. for 3 hours, and filtered. The filtered residue was washed with 30 mL of ethyl ether, and dried under vacuum to yield 1.84 g of solid paroxetine cholate as a light gray powder., 61869-08-7

As the paragraph descriping shows that 61869-08-7 is playing an increasingly important role.

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

61869-08-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in a mixed solvent of ethanol (20 mL) and isopropyl acetate (30 mL) while heating to 50 C. with shaking for 2 hours. The solution was allowed to stand at -20 C. for 48 hours, filtered, and dried under vacuum to yield 1.9 g of solid paroxetine cholate as a light gray powder.

The synthetic route of 61869-08-7 has been constantly updated, and we look forward to future research findings.

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

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, 1.0 g of oily paroxetine free base and 1.19 g of deoxycholic acid were completely dissolved in 10 mL of methyl ethyl ketone while heating to 40 C. with shaking for one hour. The solution was left to stand at -20 C.0 C. for 24 hours to precipitate a crystal, and filtered. The filtered residue was washed with cold methanol at 0 C. or below, and dried under vacuum to give 2.1 g of solid paroxetine deoxycholate as a white powder.

As the paragraph descriping shows that 61869-08-7 is playing an increasingly important role.

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

61869-08-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in a mixed solvent of methanol (10 mL) and acetone (40 mL) while heating to 40 C. with shaking for 30 minutes. The solution was allowed to stand at room temperature for 24 hours to obtain a salt. The salt was filtered, and dried under vacuum to yield 2.0 g of solid paroxetine cholate as a white crystal.

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

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, EXAMPLE 3 Preparation of paroxetine hydrochloride hemihydrate 11.58 kg of paroxetine free base was charged into a reactor containing 81.06 L of ethyl acetate and stirred for about 15 minutes at about 30 C. to form a clear solution. The reaction mass was filtered through a filtration system containing an online filter (5 micron polypropylene cloth), a 0.45 micron cartridge polypropylene filter, and a 0.2 micron cartridge polypropylene filter, and the filtration system was washed with 34.74 L of ethyl acetate. 2.895 L of 36% aqueous hydrochloric acid was added slowly to the filtrate over about 30 minutes at about 28-33 C. The reaction mass was stirred for about 1 hour, 45 minutes at about 28-30 C. It was then cooled to about 1 C. and maintained for about 1 hour, 30 minutes at about 0-2 C. The reaction mass was centrifuged and the wet cake washed with 23.16 L of chilled ethyl acetate. The wet solid was dried at 30 C. for about 1 hour, 15 minutes under a vacuum of about 690 mm Hg. The solid was further dried at about 58 C. under a vacuum of about 690 mm Hg for about 4 hours to get 10.9 kg of the paroxetine hydrochloride.; EXAMPLE 4 Purification of paroxetine hydrochloride hemihydrate 10.9 kg of the paroxetine hydrochloride obtained in Example 3 above was charged into a clean, dry reactor containing 76.3 L of acetone and the contents were heated to reflux. 4.564 L of water was added to the reaction suspension at reflux for about 60 minutes and stirred at reflux for about 20 minutes to form a clear solution. The reaction mass was cooled slowly to about 33 C. in 2 hours and then stirred for 1 hour at about 30-33 C. 32.7 L of n-heptane was charged into the reactor and stirring was continued for about 1 hour, 30 minutes. The reaction mass was cooled to about 2 C. and stirred for about 2 hours. The reaction mass was centrifuged and wet cake was washed with 6.54 L of chilled acetone. The wet solid was dried under vacuum of about 690 mm Hg at about 30 C. for about 2 hours and then at about 55-57 C. for about 4 hours. The resultant solid was milled in a micronizer (Manufacturer: Microtech Engineering company, Model: M-50) with an air pressure of 0.5 kg/cm2 at a feed rate of 7 kg/hour and then sieved through a 10 mesh sieve yielding 8.7 Kg of paroxetine hydrochloride hemihydrate with particle size distribution: D10=2.37 mum; D50=11.1 mum; and D90=30.6 mum.

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; Thippannachar, Vijayavitthal Mathad; Jayantilal, Pravinchandra Vankawala; Elati, Chandrasekhar Ravi Ram; Kolla, Naveen Kumar; Chlamala, Subrahmanyeswara Rao; US2006/264637; (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.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.,61869-08-7

203-L isopropanol (water 0. 05% w/v) and 13.5 Kg Paroxetine base are charged simultaneously in a reactor and stirred for 15 min to get clear solution. The solution is filtered through sparkler filter to remove suspended particles. The reactor and sparkler filters are washed with 2 x 13.5-L isopropanol. The filtrate and washing solutions are collected into a glass-lined reactor. To this solution of Paroxetine base a solution of 20% w/v hydrogen chloride in isopropanol is added from addition funnel during 120 minutes at 30-35C to bring the pH of the reaction mass between 3-4 (checked on pH paper), at this pH Paroxetine hydrochloride crystallizes. The slurry is stirred for 15 minutes and then slowly heated to 80-82C, 135 L isopropanol is distilled off at atmospheric pressure and then cooled. The product crystallized out at 45C, which is then further cooled to 30-35C and stirred for 1 hr at this temperature. The product is centrifuged and washed with 2 x 13.5-L isopropanol. The wet cake is then transferred to a vacuum tray dryer. The product is dried at 30-35C for 2 hrs, at 50-55C for 6 hrs and finally at 70-75C for 12 hrs under reduced pressure of 30 mm, reducing isopropanol content to less than 3%. The yield of anhydrous Paroxetine hydrochloride is 13.5 Kg Water content of distillate 0.6% Melting point 116-117C Purity (by HPLC) 99.72% Water (by KFR) 1.48% isopropanol (by GC) 2.4%; Example 2 20 g of Paroxetine base is dissolved in 360-ml isopropanol (water <0.05%). The solution is filtered through filter pad in Buchner funnel. The pad is washed twice with 20-ml isopropanol. To the clear filtrate is added 20% w/v hydrogen chloride solution in isopropanol at 30-35C to bring the pH of the reaction mass between 3-4 (checked on pH paper). Paroxetine hydrochloride is CRYSTALLISED out. The slurry is stirred for 15 minutes and then slowly heated to 80-82C to obtain a clear solution, which is then subjected to distillation for the removal of 200 ml isopropanol at atmospheric pressure. The solution is then cooled and the product crystallised out at 30-35C. Slurry thus obtained is stirred for 1 hr at the same temperature. The product is filtered and washed with 4 x 20-ml isopropanol. The wet cake is dried in vacuum oven at 65C for 4 hrs and between the range 70-75C for 16 hrs under reduced pressure of 30 mm to afford 19.9 g Paroxetine hydrochloride. Melting point 116-117C Water content of distillate 0.55% Purity by HPLC 99.96%, Isopropanol (by GC) 2.96% Water (by KFR) 1.5%; Example 3 20 g of Paroxetine base is dissolved in 360-ml isopropanol (water <0.05%). The solution is filtered through filter pad in Buchner funnel. The pad is washed twice with 20 ml isopropanol. To the clear filtrate is added 20% hydrogen chloride solution in isopropanol at 30-35C to bring the pH of the reaction mass between 3-4 (checked on pH paper). Paroxetine hydrochloride is crystallized out at this pH. The slurry is stirred for 15 min. and then slowly heated to 80-82C to obtain a clear solution, which is then subjected to distillation for removal of 200 ml isopropanol at atmospheric pressure. The solution is then cooled to 30 to 35 C and the product crystallized out. The slurry thus obtained is stirred for 1 hour. The product is filtered and washed with 4 x 20-ml isopropanol. The wet cake is dried in vacuum oven between the range 70-75C for 16 hrs under reduced pressure of 30 mm to afford 19.5 g of Paroxetine hydrochloride. Melting point 116-117C Water content of distillate 0.6% Purity by HPLC 99.96%, Isopropanol (by GC) 2.18% Water (by KFR) 1.46% The synthetic route of 61869-08-7 has been constantly updated, and we look forward to future research findings. Reference：
Patent; CADILA HEALTHCARE LIMITED; WO2005/19209; (2005); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem