实验室的空气污染和爆炸事故

根据实践经验，对化学实验室的空气污染和爆炸事故提出了注意事项和防范措施。     

柔红酮和阿霉酮二肽衍生物的合成

本文报道柔红酮和阿霉酮二肽衍生物的合成。二肽与柔红酮在DCC/DMAP或苯磺酰氯/吡啶存在下反应,得到柔红酮衍生物,继之溴化、水解得到阿霉酮衍生物或直接由二肽与保护阿霉酮酯化,脱保护后得到阿霉酮衍生物。合成的18个化合物对L₁₂₁₀白血病细胞增殖均有抑制作用,并存在一定的构效关系,游离氨基的位置与抗肿瘤活性相关。     

Antitumor Agents 126. Novel 4β-Substituted Anilino Derivatives of 3′,4′ -O,O-Didemethylpodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II

A series of derivatives of 3,4 0,0-didemethylpodophyllotoxin have been synthesized and evaluated for their inhibitor activity against neoplastic cell growth (KB) and against human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. The results show that the compounds possessing a 4-anilino moiety either unsubstituted or substituted at the para (F, COOCH₃, COCH₃, CN, CH₂CN, NO₂) or meta (OH) positions or with an ethylenedioxy moiety showed the same or greater activity than etoposide in causing cellular protein-linked DNA breakage and in inhibiting DNA topoisomerase II. However, compared to the corresponding 4-0-demethyl analogues, the 3,4-O,O-didemethyl compounds have a similar potency in inhibition of DNA topoisomerase II but are less active in causing cellular protein-linked DNA breakage. Complete correlation between the three biological activities–cytotoxicity, inhibition of DNA topoisomerase II, and induction of protein-linked DNA breakage–was also not observed. This supports the possibility that the biological determinants of action among these compounds may be different.     

慎用化学致癌物质

介绍了美国国立环境卫生研究院在2001年发布的第9次致癌物质报告,共计有200多种化合物已知有肯定或可疑的致癌作用,供药物化学工作者参考,以加强劳动保护和确保药品质量.     

Meta-analysis of laparoscopy assisted distal gastrectomy and conventional open distal gastrectomy for EGC

In recent decades, laparoscopy assisted distal gastrectomy (LADG) has been introduced to treat early gastric cancer (EGC). This study evaluated the safety and efficacy of laparoscopy assisted and conventional open distal gastrectomy for EGC. Comprehensive searches of PubMed, EmBase, Cochrane Controlled Trials Register and Chinese Biomedical Database (CBM) were performed. Included literature was evaluated using the Newcastle-Ottawa Scale. Original data were extracted, pooled odds ratio (OR) and 95% confidence intervals (CI) were calculated using RevMan 5.0. Eight RCTs of 734 patients were included in the study. Compared to CODG, LADG increases the operation time (weighted mean difference [WMD]: 63.35; 95% confidence interval [CI]: 57.96, 68.74; P < 0.01), reduces intraoperative blood loss (WMD: ?127.95; 95% CI: ?147.97, ?107.93; P < 0.01), decreases number of harvested lymph nodes (WMD: ?4.21; 95% CI: ?6.10, ?2.31; P < 0.01), forwards oral intake time (WMD:?0.43; 95% CI: ?0.61, ?0.24; P < 0.01), and shortens hospital stay(WMD: ?1.29; 95% CI: ?1.76, ?0.83; P < 0.01). There is no significant difference in postoperative complications(OR: 0.70; 95% CI: 0.46, 1.06; P = 0.09). All these findings indicate that LADG for EGC is feasible and safe.     

实用高效的酰胺键形成试剂

HOAt、HOBt和6-Cl-HOBt是高效实用的酰胺键形成促进剂。它们能防止或大幅减少消旋反应，抑制副产物的产生。在制备、运输、应用及废料处理中要注意安全，防止爆炸。     

一种合成蒽环酮的新中间体:(±)-2-乙基-2-羟基-7-溴-5,8-二甲氧基-1,2,3,4-四氢萘

报道一种合成蒽环酮的新方法。以α-卤醇(12)为中间体,在碱性条件下脱去卤化氢形成环氧化物13,继而引入蒽环酮C-9位羟基。各步收率达75％以上。     

用β-羰基羧酸酯制备其酰胺的简便方法

为提供公斤级的N-对氟苄基-2（1H）-喹诺酮-3-甲酰胺，经几种合成方法的比较试验，找到一条从2（1H）-喹诺酮-3-羧酸乙脂与对氟苄胺反应，直接一步合成的方法。145C反应2h，收率96％。用同一方法制备了50多个类似化合物。     

药物多晶型与有效性

讨论了药物多晶型对理化性质、生物利用度、相关制剂的影响.介绍了药物多晶型的检测技术,及在新药研发和申请专利保护时的重要性,并举例说明了最佳晶型的优选.     

(±)-2-甲基-2-羟基-5,8-二甲氧基-1,2,3,4-四氢萘的简便合成法

报道蒽环酮关键中间体AB环的一种简便合成方法。从对苯醌和异戊二烯起始,经Diels-Alder加成、甲基化、羟基化三步反应,以总收率58％得到(±)-2-甲基-2-羟基-5,8-二甲氧基-1,2,3,4-四氢萘。这是迄今已报道的路线中较为简捷的一条。