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µÚÒ»¾ä£ºIn order to determination of lamivudine and its
related substances by HPLC and study the structure-activity relationships of oxathiolanyl
nucleosides as potential anti-virus agents, the synthesis geometrical isomer cis-(¡À) 1 and
trans-(¡À) 2 of lamivudine was needed.

µÚ¶þ¾ä£ºThe mixture was separated by silica gel column chromatography
using EtOAc/MeOH (50:1) as eluant to achieved 8 in 58% yield as the slow moving
component7 and 9 in 25% yield as the fast moving product8 (Lit.5 8 and 9 combined yield
55.3%). Deprotection of 8 and 9 using NH4OH in EtOH at room temperation produced
the desired cis-(¡À) 19 and trans-(¡À) 210 in 84.7% and 92.5% yield, respectively.

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ringzhu(½ð±Ò+20, ·­ÒëEPI+1): ~~ 2011-03-26 15:01:34
ÒýÓûØÌû:
Originally posted by wight3 at 2011-03-02 11:50:29:
µÚÒ»¾ä£ºIn order to determination of lamivudine and its
related substances by HPLC and study the structure-activity relationships of oxathiolanyl
nucleosides as potential anti-virus agents, the s ...

1.ΪÁËͨ¹ýHPLC¼ì²âÀ­Ã×·ò¶¨¼°Óë´ËÏà¹ØµÄÎïÖÊÒÔ¼°Ñо¿ÑõÁòÔÓ»·Îì»ùºËÜÕ×÷Ϊ¿¹²¡¶¾Ò©¼ÁµÄ½á¹¹»îÐÔ£¬ÎÒÃÇÐèÒªºÏ³ÉÀ­Ã×·ò¶¨µÄÕýʽºÍ·´Ê½Í¬·ÖÒì¹¹Ìå¡£
2Â¥2011-03-02 12:21:11
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï ¡ï
ringzhu(½ð±Ò+20): ~~ 2011-03-26 15:01:42
»ìºÏÎïÔڹ轺Öù²ãÎö£¨Ï´ÍѼÁ£ºEtOAc/MeOH (50:1)£©Ï´ÍÑϵõ½»¯ºÏÎï8£¨²úÂÊ58%£©£¬¶øºóÏ´ÍÑÏÂÀ´µÄ7ºÍ9²úÂÊΪ25%£¬ÏÈÏ´ÍÑÏÂÀ´µÄ²úÎïΪ8£¨8ºÍ9×ܲúÂÊΪ55.3%£©¡£8ºÍ9ÔÚNH4OHµÄEtOHÈÜÒºÖÐÊÒÎÂÍѱ£µÃµ½ËùÐèµÄcis-(¡À) 19£¨²úÂÊΪ84.7%£© ÒÔ¼° trans-(¡À) 210£¨²úÂÊΪ92.5%£©
3Â¥2011-03-02 12:22:44
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
In order to£¨¸öÈ˾õµÃÕâ¸ö¾ä×ÓÓÉ´íÎó£¬Ó¦¸ÃÓÃFOR£© determination of lamivudine and its
related substances by HPLC and study the structure-activity relationships of oxathiolanyl
nucleosides as potential anti-virus agents, the synthesis geometrical isomer cis-(¡À) 1 and
trans-(¡À) 2 of lamivudine was needed.
ΪÁËͨ¹ýHPLC¼ì²âÀ­Ã×·ò¶¨¼°Óë´ËÏà¹ØµÄÎïÖÊÒÔ¼°Ñо¿ÑõÁòÔÓ»·Îì»ùºËÜÕ×÷Ϊ¿¹²¡¶¾Ò©¼ÁµÄ¹¹Ð§¹ØÏµ£¨SAR£©£¬ÎÒÃÇÐèÒªºÏ³ÉÀ­Ã×·ò¶¨µÄÕýʽͬ·ÖÒì¹¹Ìå¡£
4Â¥2011-03-02 12:26:41
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
ÒýÓûØÌû:
Originally posted by wight3 at 2011-03-02 11:50:29:
µÚÒ»¾ä£ºIn order to determination of lamivudine and its
related substances by HPLC and study the structure-activity relationships of oxathiolanyl
nucleosides as potential anti-virus agents, the s ...

2.»ìºÏÎïͨ¹ý¹è½º²ãÎö·ÖÀ룬ÓÃEtOAc/MeOH (50:1)×÷ΪϴÍѼÁµÃµ½²úÂÊ58%µÄµÍÁ÷¶¯×é·Ö8ÒÔ¼°²úÂÊ25%µÄ¿ìÁ÷¶¯×é·Ö7ºÍ9£¨8ºÍ9Ò»ÆðµÄµÃÂÊΪ55.3%£©¡£Í¨¹ýNH4OHºÍEtOHÔÚÊÒÎÂÏÂÍÑÏ´µÃµ½8ºÍ9£¬·´Ê½Òì¹¹Ìå19ºÍÕýʽÒì¹¹Ìå210µÄµÃÂÊ·Ö²¼Îª84.7%ºÍ92.5%¡£
5Â¥2011-03-02 12:29:59
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
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