公开(公告)号：EP1095047B1

公开(公告)日：2005-07-27

申请号：EP00930305.8

申请日：2000-05-03

Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA

Inventor： MCKENNA, Charles, E. ,  LI, Zengmin

IPC: 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: 公开并要求保护的用于将亚磷酸酯或膦酸酯转化为相应的硫代亚磷酸酯或硫代膦酸酯并用于合成如此制备的特定硫代亚磷酸酯和硫代膦酸酯化合物的改进方法。 该方法从使用P4S10作为硫化试剂的亚磷酸二酯开始。 将反应混合物回流直至反应完成，然后分离和氯甲酸酯磷酸酯化步骤以产生纯的硫代膦酰基羧酸酯三酯。 或者，这些酯可直接通过P4S10作用于相应的膦酰基羧酸酯来制备。 前一种方法用于制备硫代亚磷酸二甲酯，然后是三甲基硫代膦酰基甲酸酯，它是合成硫代膦酰甲酸盐的关键中间体，其具有抗病毒性质。

公开(公告)号：EP1095047A1

公开(公告)日：2001-05-02

申请号：EP00930305.8

申请日：2000-05-03

Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA

Inventor： MCKENNA, Charles, E. ,  LI, Zengmin

IPC: C07F9/16

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: 公开并要求保护的用于将亚磷酸酯或膦酸酯转化为相应的硫代亚磷酸酯或硫代膦酸酯并用于合成如此制备的特定硫代亚磷酸酯和硫代膦酸酯化合物的改进方法。 该方法从使用P4S10作为硫化试剂的亚磷酸二酯开始。 将反应混合物回流直至反应完成，然后分离和氯甲酸酯磷酸酯化步骤以产生纯的硫代膦酰基羧酸酯三酯。 或者，这些酯可直接通过P4S10作用于相应的膦酰基羧酸酯来制备。 前一种方法用于制备硫代亚磷酸二甲酯，然后是三甲基硫代膦酰基甲酸酯，它是合成硫代膦酰甲酸盐的关键中间体，其具有抗病毒性质。