Tiofēnu saturošu termošoka proteīna Hsp90 inhibitoru sintēzes pētījumi
Date
2006
Authors
Sizovs, Antons
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Publisher
Latvijas Universitāte
Abstract
Darbā ir izdarīts mēģinājums izstrādāt metodes 6-arilmetil-7-alkiltiēno[3,2-d]pirimidīn-4-amīnu un 3,4-asimetriski aizvietotu tiofēnu sintēzei. Ir parādīts, ka vienas no piedāvātām 6-arilmetil-7-alkiltiēno[3,2-d]pirimidīn-4-amīnu sintēzes shēmām no 3,4,5-trimetoksietānskābes praktiska realizācija nav iespējama; otras shēmas – 6-arilmetil-7-alkiltiēno[3,2-d]pirimidīn-4-amīnu sintēze no metil 3-aminotiofēn-2-karboksilāta – praktiska pārbaude šī darba ietvaros netika pabeigta. Ir atrasti apstākļi Suzuki-Mijauras reakcijai, kuros ir izdevies iegūt 3-brom-4-arilaizvietotus tiofēna atvasinājumus no 3,4-dibromtiofēna, kuri tālāk izmantoti 3,4-asimetriski diarilaizvietotu tiofēnu sintēzei. Iespējams, ka atrastos apstākļos var realizēt daudzu līdzīgu 3,4-asimetriski aizvietotu tiofēna atvasinājumu sintēzi.
An attempt to elaborate methods of synthesis of 6-arylmethyl-7-alkylthieno[3,2-d]pyrimidin-4-amines and 3,4-unsymmetrically arylsubstituted thiophenes has been undertaken. It was shown, that one of the purposed schemes of synthesis of 6-arylmethyl-7-alkylthieno[3,2-d]pyrimidin-4-amines starting from 3,4,5-trimethoxyphenylacetic acid cannot be practically implemented; the second of the purposed schemes – synthesis of 6-arylmethyl-7-alkylthieno[3,2-d]pyrimidin-4-amines from methyl 3-aminothiophene-2-carboxylate has not been finished. The reaction conditions of Suzuki-Miyaura reaction suitable for the preparation of 3-bromo-4-arylsubstituted thiophenes from 3,4-dibromothiophene, which were then used for further synthesis of 3,4-usymmetrically arylsubstituted thiophene derivatives, have been found.
An attempt to elaborate methods of synthesis of 6-arylmethyl-7-alkylthieno[3,2-d]pyrimidin-4-amines and 3,4-unsymmetrically arylsubstituted thiophenes has been undertaken. It was shown, that one of the purposed schemes of synthesis of 6-arylmethyl-7-alkylthieno[3,2-d]pyrimidin-4-amines starting from 3,4,5-trimethoxyphenylacetic acid cannot be practically implemented; the second of the purposed schemes – synthesis of 6-arylmethyl-7-alkylthieno[3,2-d]pyrimidin-4-amines from methyl 3-aminothiophene-2-carboxylate has not been finished. The reaction conditions of Suzuki-Miyaura reaction suitable for the preparation of 3-bromo-4-arylsubstituted thiophenes from 3,4-dibromothiophene, which were then used for further synthesis of 3,4-usymmetrically arylsubstituted thiophene derivatives, have been found.
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