公开(公告)号：US20160237077A1

公开(公告)日：2016-08-18

申请号：US15028962

申请日：2014-10-16

Applicant: PROCOS S.P.A.

Inventor： Tommaso Angelini ,  Piergiorgio Bettoni ,  Jacopo Roletto ,  Paolo Paissoni

IPC: C07D417/12

CPC classification number: C07D417/12

Abstract: Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1-yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7-methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.

Abstract translation: 公开了从（1R，2R） - 环己烷-1,2-二基二甲醇（1），3-（哌嗪-1-基）苯并[d]异噻唑（3）和（3aR，4R）的工业合成卢拉西坦的方法 ，7R，7aS）-3a，4,7,7a-四氢-4,7-甲烷异苯并呋喃-1,3-二酮（6））。 所述方法被优化以通过制备高纯度的合成中间体来获得具有高产率和高纯度的Lurasidone，使用临近的原料和试剂，其量接近化学计量量，提高生产率并降低该方法的成本和环境影响。

公开(公告)号：US09518047B2

公开(公告)日：2016-12-13

申请号：US15028962

申请日：2014-10-16

Applicant: PROCOS S.P.A.

Inventor： Tommaso Angelini ,  Piergiorgio Bettoni ,  Jacopo Roletto ,  Paolo Paissoni

IPC: C07D417/12

CPC classification number: C07D417/12

Abstract: Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1-yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7-methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.

公开(公告)号：US20190010141A1

公开(公告)日：2019-01-10

申请号：US16066328

申请日：2016-12-22

Applicant: Procos S.P.A.

Inventor： Martino Veronese ,  Piergiorgio Bettoni ,  Jacopo Roletto ,  Paolo Paissoni

IPC: C07D401/06

Abstract: Disclosed is a process for the synthesis of efinaconazole (I), starting from 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole and 4-methylenepiperidine, as free base or hydrochloride, in an organic solvent, under anhydrous conditions and in the presence of neutralising agents and reaction-promoting metal species. (1) The process is particularly advantageous because it gives rise to efinaconazole in high yields and purity, and uses little more than the stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.