²©Ô´¹ú¼Ê

ÐÂÎŶ¯Ì¬

ÑǼװ·Ò¶Á¢µÂ½éµ¼µÄ[3+2]»·¼Ó³É£ºN-(¼×Ñõ¼×»ù)-N-(Èý¼×»ù¹è¼×»ù)Üа·µÄ½¹µã×÷ÓÃ
·ÖÀà £ºÐÂÎÅ
Ðû²¼Ê±¼ä £º2024/08/27
»á¼ûÁ¿ £º

º¬µªÔÓ»·À໯ºÏÎïÊÇÒ»ÀàÖ÷ÒªµÄÔÓ»·»¯ºÏÎï £¬ÔÚÓлú»¯Ñ§ÁìÓòÕ¼ÓÐ×ÅÖ÷Ҫְλ¡£ÔÚÒ½Ò©ÁìÓò £¬µªÔÓ»·»¯ºÏÎï×é³ÉÁËÐí¶àÒ©Îï·Ö×ӵĽ¹µã½á¹¹£¨¼ûͼһ£© £¬ËüÃǹØÓÚÖÎÁÆÖÖÖÖ¼²²¡¾ßÓв»¿ÉÌæ»»µÄ×÷Ó᣾Ýͳ¼Æ £¬ÃÀ¹úʳÎïÒ©Æ·¼àÊÓ¹ÜÀí¾Ö£¨FDA£©Åú×¼µÄÒ©ÎïÖÐ £¬Ò»°ëÒÔÉϰüÀ¨ÖÁÉÙÒ»¸öµªÔÓ»·½á¹¹¡£±ðµÄ £¬º¬µªÔÓ»·»¯ºÏÎï £¬ÔÚũҵ¡¢È¾ÁÏÖÆÔìÒÔ¼°Ó°ÏñÊÖÒÕµÈÐÐÒµ £¬Í¬Ñùʩչ×ÅÖ÷ÒªµÄ×÷Óà £¬ÏÔʾ³öÆäÆÕ±éµÄÓ¦ÓüÛÖµºÍÖ÷ÒªÐÔ¡£


Ê×Ò³_²©Ô´¹ú¼ÊÍøÕ¾

ͼһ º¬µªÔÓ»·Ò©Îï

º¬µªÔÓ»·»¯ºÏÎïµÄºÏ³ÉÒªÁìÓÐÐí¶à £¬°üÀ¨»·¼Ó³É·´Ó¦¡¢»¯Ñ§Ã¸·¨ºÏ³É¡¢²î³Ø³Æ´ß»¯¡¢ÓлúµçºÏ³ÉµÈ¡£ÆäÖÐ £¬»·¼Ó³É·´Ó¦ÊÇÓÃÀ´¹¹½¨´ËÀ໯ºÏÎïµÄ³£ÓÃÒªÁì¡£N-(¼×Ñõ¼×»ù)-N-(Èý¼×»ù¹è¼×»ù)Üа·ÊÇÒ»ÖÖ1,3-ż¼«×Ó £¬¿ÉÒÔÔÚÈý·úÒÒËá¡¢TBAFµÈ´ß»¯¼ÁµÄ×÷ÓÃÏÂԭλÌìÉúÒ»ÖÖÑǼװ·ÐÍÒ¶Á¢µÂ £¬½ø¶øÓëÇ׿¼«Ì屬·¢[3+2]»·¼Ó³É·´Ó¦ £¬»ñµÃÎåÔªµªÔÓ»·»¯ºÏÎï¡£ÖµµÃÒ»ÌáµÄÊÇ £¬¸Ã·´Ó¦ÓëÁ´×´Ï©Ìþ·´Ó¦ÌåÏÖ³öÍêÈ«µÄ˳ʽÁ¢ÌåÑ¡ÔñÐÔ £¬ÕâÒâζ×Å·´Ó¦Àú³ÌÖмá³ÖÁË·Ö×ÓÖÐÔ­ÓеÄÏà¶ÔÁ¢Ìå¹¹ÐÍ £¬ÕâÒ»ÌØÕ÷¹ØÓںϳɾßÓÐÌØ¶¨¿Õ¼ä½á¹¹µÄÖØ´ó·Ö×Ó¾ßÓÐÖ÷ÒªÒâÒå¡£Èçͼ¶þËùʾ£º


ͼ¶þ ÓëÁ´×´Ï©ÌþµÄ»·¼Ó³É·´Ó¦


±ðµÄ £¬ÔÚN-(¼×Ñõ¼×»ù)-N-(Èý¼×»ù¹è¼×»ù)Üа·¼ÓÈëµÄ[3+2]»·¼Ó³É·´Ó¦ÖÐ £¬ÔÚÓ뺬Óл·×´½á¹¹µÄÏ©Ìþ·´Ó¦Ê±Õ¹ÏÖ³öÁËÓÅÒìµÄ·Ç¶ÔӳѡÔñÐÔ £¬ÕâÒ»ÌØÕ÷¹ØÓڽṹ¾ßÓÐÖØ´ó¿Õ¼ä¹¹Ð͵ķÖ×ÓÖÁ¹ØÖ÷Òª¡£Ïêϸ¶øÑÔ £¬Óë»·Ï©£¨Ë«¼üÔÚ»·ÄÚ£©·´Ó¦Ê±»áÌìÉú³í»·»¯ºÏÎï £¬¶øÓë»·ÍâË«¼ü£¨Óë»·ÏàÁ¬£©·´Ó¦Ê±Ôò»áÌìÉúÂÝ»·»¯ºÏÎï £¬ÕâÖÖ·´Ó¦ÌØÕ÷¿ÉÒÔÑ¡ÔñÐԵĹ¹½¨Ìض¨ÀàÐ͵Ļ·×´½á¹¹ £¬ÈçͼÈýËùʾ£º


Ê×Ò³_²©Ô´¹ú¼ÊÍøÕ¾

ͼÈý Ó뺬»·Ï©ÌþµÄ»·¼Ó³É·´Ó¦


ÖµµÃÒ»ÌáµÄÊÇ £¬N-(¼×Ñõ¼×»ù)-N-(Èý¼×»ù¹è¼×»ù)Üа·ËùÐγɵÄÑǼװ·ÐÍÒ¶Á¢µÂ²»µ«¿ÉÒÔÓë̼̼˫¼ü·´Ó¦³É»· £¬»¹¿ÉÒÔÓëôÊ»ù±¬·¢»·¼Ó³É·´Ó¦ÖƱ¸‡fßòÍéÀ໯ºÏÎï £¬ÈçͼËÄËùʾ£ºÔÚ·ú»¯ï®µÄ´ß»¯ÏÂN-(¼×Ñõ¼×»ù)-N-(Èý¼×»ù¹è¼×»ù)Üа·Óë²î±ðÀàÐ͵ÄÖ¬·¾È©·´Ó¦ÒÔ²»´íµÄÊÕÂÊ»ñµÃÏìÓ¦µÄ‡fßòÍ黯ºÏÎï¡£


Ê×Ò³_²©Ô´¹ú¼ÊÍøÕ¾

ͼËÄ ÓëÖ¬·¾È©µÄ»·¼Ó³É·´Ó¦


N-(¼×Ñõ¼×»ù)-N-(Èý¼×»ù¹è¼×»ù)Üа·ÊÇ»·¼Ó³É·´Ó¦Öг£ÓõÄÒ»ÖÖÊÔ¼Á £¬ÆÕ±éÓ¦ÓÃÓںϳɶàÈ¡´úµÄßÁ¿©Í黯ºÏÎïºÍÒ½Ò©ÖÐÐÄÌå¡£¸Ã»¯ºÏÎïͨ³£ÊÇͨ¹ýN-(Èý¼×¹è»ù¼×»ù)Üа·Óë¼×È©ºÍ¼×´¼·´Ó¦»ñµÃ¡£ÖÊÁÏN-(Èý¼×¹è»ù¼×»ù)Üа·Ò²ÊÇÒ»ÖÖÖ÷ÒªµÄÓлúºÏ³ÉÖÐÐÄÌå £¬¿ÉÒÔÓëÈ©µÈÊÔ¼Á £¬¾ÙÐÐÈý×é·Ö·´Ó¦Ö±½Ó¹¹½¨ÔÓ»·»¯ºÏÎï £¬»¹¿ÉÒÔÓÃÓںϳɵªÔÓ»·µÄ¸¬°±ËáëÄ £¬ÈçͼÎåËùʾ£º


Ê×Ò³_²©Ô´¹ú¼ÊÍøÕ¾

ͼÎå º¬µªÔÓ»·¸¬°±ËáëĵĺϳÉõè¾¶





²Î¿¼ÎÄÏ×

[1] Amin, A.; Qadir, T.; Abe, H.; et al. A Review on The Medicinal And Industrial Applications of N-Containing Heterocycles[J]. The Open Medicinal Chemistry Journal, 2022, 16.

[2] Kumar, A.; Singh, A.K.; Kumar, P.; et al. Nitrogen Containing Heterocycles as Anticancer Agents: AMedicinal Chemistry Perspective[J]. Pharmaceuticals, 2023, 16, 299.

[3] N-Benzyl-N-(methoxymethyl)-N-trimethylsilylmethylamine. Encyclopedia of Reagents for Organic Synthesis, 2001.

[4] Gorbunova, E.; Buev, E.M.; Moshkin, V.S.; et al. Three Ways Aliphatic Aldehydes React with Nonstabilized Azome thine Ylides[J]. SynLett, 2020, 31.

[5] ÁõÑÒ, Ì·¹ã»Û, ½ðӢѧµÈ. ¹âÓÕµ¼µ¥µç×Ó×ªÒÆ·´Ó¦ºÏ³ÉµªÔÓ»·¸¬°±ËáëÄ[J]. Óлú»¯Ñ§, 2011, 31, 480-485.




ÍøÕ¾µØÍ¼