公开(公告)号：ES2244442T3

公开(公告)日：2005-12-16

申请号：ES00930305

申请日：2000-05-03

Applicant: UNIV SOUTHERN CALIFORNIA

Inventor： MCKENNA CHARLES E ,  LI ZENGMIN

IPC: C07F9/201 ,  C07F9/40 ,  C07F9/16 ,  C07F9/165

Abstract: Un método para la preparación de ésteres de tiofosfito de fórmula en que el método comprenda los pasos de: (a) la formación de una mezcla de reacción de un éster de fosfonoformato de fórmula una cantidad efectiva de pentasulfuro de fósforo, y un disolvente adecuado, dónde R1, R2 y R3 son cada uno alquilo, alquenilo, alquinilo, o arilo sustituido o insustituido o un grupo protector adecuado; y (b) el calentamiento de dicha mezcla de reacción a una temperatura adecuada hasta que la conversión del éster de fosfonoformato (4) a éster de tiofosfonoformato (3) sea sustancialmente completa.

公开(公告)号：AT300548T

公开(公告)日：2005-08-15

申请号：AT00930305

申请日：2000-05-03

Applicant: UNIV SOUTHERN CALIFORNIA

Inventor： MCKENNA CHARLES E ,  LI ZENGMIN

IPC: C07F9/201 ,  C07F9/40 ,  C07F9/16 ,  C07F9/165

Abstract: Improved methods for converting phosphite or phosphonate esters into corresponding thiophosphites or thiophosphonates and for synthesizing specific thiophosphite and thiophosphonate compounds so produced are disclosed and claimed. The methods start from phosphite diesters using P4S10 as the thionation reagent. The reaction mixture is refluxed until the reaction is complete and may be followed by separation and chloroformate ester phosphonation steps to produce pure thiophosphonocarboxylate triesters. Alternatively, these esters may be prepared directly by action of P4S10 on the corresponding phosphonocarboxylate esters. The former method was used to prepare dimethyl thiophosphite and thence trimethyl thiophosphonoformate, a key intermediate in synthesis of salts of thiophosphonoformic acid, which have anti-viral properties.

公开(公告)号：DE60021500T2

公开(公告)日：2006-05-24

申请号：DE60021500

申请日：2000-05-03

Applicant: UNIV SOUTHERN CALIFORNIA

Inventor： MCKENNA E ,  LI ZENGMIN

IPC: C07F9/16 ,  C07F9/165 ,  C07F9/201 ,  C07F9/40

Abstract: Improved methods for converting phosphite or phosphonate esters into corresponding thiophosphites or thiophosphonates and for synthesizing specific thiophosphite and thiophosphonate compounds so produced are disclosed and claimed. The methods start from phosphite diesters using P4S10 as the thionation reagent. The reaction mixture is refluxed until the reaction is complete and may be followed by separation and chloroformate ester phosphonation steps to produce pure thiophosphonocarboxylate triesters. Alternatively, these esters may be prepared directly by action of P4S10 on the corresponding phosphonocarboxylate esters. The former method was used to prepare dimethyl thiophosphite and thence trimethyl thiophosphonoformate, a key intermediate in synthesis of salts of thiophosphonoformic acid, which have anti-viral properties.

公开(公告)号：DE60021500D1

公开(公告)日：2005-09-01

申请号：DE60021500

申请日：2000-05-03

Applicant: UNIV SOUTHERN CALIFORNIA

Inventor： MCKENNA E ,  LI ZENGMIN

IPC: C07F9/201 ,  C07F9/40 ,  C07F9/16 ,  C07F9/165

Abstract: Improved methods for converting phosphite or phosphonate esters into corresponding thiophosphites or thiophosphonates and for synthesizing specific thiophosphite and thiophosphonate compounds so produced are disclosed and claimed. The methods start from phosphite diesters using P4S10 as the thionation reagent. The reaction mixture is refluxed until the reaction is complete and may be followed by separation and chloroformate ester phosphonation steps to produce pure thiophosphonocarboxylate triesters. Alternatively, these esters may be prepared directly by action of P4S10 on the corresponding phosphonocarboxylate esters. The former method was used to prepare dimethyl thiophosphite and thence trimethyl thiophosphonoformate, a key intermediate in synthesis of salts of thiophosphonoformic acid, which have anti-viral properties.

公开(公告)号：CA2336605A1

公开(公告)日：2000-11-09

申请号：CA2336605

申请日：2000-05-03

Applicant: UNIV SOUTHERN CALIFORNIA

Inventor： LI ZENGMIN ,  MCKENNA CHARLES E

IPC: C07F9/201 ,  C07F9/40 ,  C07F9/16

Abstract: Improved methods for converting phosphite or phosphonate esters into corresponding thiophosphites or thiophosphonates and for synthesizing specif ic thiophosphite and thiophosphonate compounds so produced are disclosed and claimed. The methods start from phosphite diesters using P4S10 as the thionation reagent. The reaction mixture is refluxed until the reaction is complete and may be followed by separation and chloroformate ester phosphonation steps to produce pure thiophosphonocarboxylate triesters. Alternatively, these esters may be prepared directly by action of P4S10 on t he corresponding phosphonocarboxylate esters. The former method was used to prepare dimethyl thiophosphite and thence trimethyl thiophosphonoformate, a key intermediate in synthesis of salts of thiophosphonoformic acid, which ha ve anti-viral properties.

公开(公告)号：EP1095047A4

公开(公告)日：2002-05-15

申请号：EP00930305

申请日：2000-05-03

Applicant: UNIV SOUTHERN CALIFORNIA

Inventor： MCKENNA CHARLES E ,  LI ZENGMIN

IPC: C07F9/201 ,  C07F9/40 ,  C07F9/16 ,  C07F9/165

CPC classification number: C07F9/4065 ,  C07F9/201

Abstract: Improved methods for converting phosphite or phosphonate esters into corresponding thiophosphites or thiophosphonates and for synthesizing specific thiophosphite and thiophosphonate compounds so produced are disclosed and claimed. The methods start from phosphite diesters using P4S10 as the thionation reagent. The reaction mixture is refluxed until the reaction is complete and may be followed by separation and chloroformate ester phosphonation steps to produce pure thiophosphonocarboxylate triesters. Alternatively, these esters may be prepared directly by action of P4S10 on the corresponding phosphonocarboxylate esters. The former method was used to prepare dimethyl thiophosphite and thence trimethyl thiophosphonoformate, a key intermediate in synthesis of salts of thiophosphonoformic acid, which have anti-viral properties.

Abstract translation: 将亚磷酸酯或膦酸酯转化成相应的硫代亚磷酸酯或硫代膦酸酯并合成如此生产的特定硫代亚磷酸酯和硫代膦酸酯化合物的改进方法被公开和要求保护。 方法从使用P4S10作为硫化试剂的亚磷酸二酯开始。 将反应混合物回流直到反应完成，然后分离和氯甲酸酯膦酸化步骤以产生纯的硫代膦酰基羧酸酯三酯。 或者，这些酯可以直接通过P4S10在相应的膦酰基羧酸酯上的作用来制备。 使用前一种方法制备二硫代亚磷酸二甲酯，然后制备硫代膦酰甲酸三甲酯，这是合成硫代膦酰甲酸盐的关键中间体，具有抗病毒性质。