CAS: 2401-21-0; 1,2-Dichloro-3-Iodobenzene

邻二氯苯置于li(2,2,6,6-Tetramethylpiperidide)*al(Ibu)3,碘体系中,用 四氢呋喃,正己烷 用作溶剂,化学反应 6.0H,以72%的收率获得2,3-二氯碘苯
参考文献:使用铝酸碱区域选择性和化学选择性直接生成官能化芳香铝化合物
标题:使用铝酸碱区域选择性和化学选择性直接生成官能化芳香铝化合物
摘要:使用三异丁基(四甲基哌啶基)铝酸盐 (Ibu3Al(Tmp)Li) 通过去质子定向邻位铝化生成官能化芳族铝化合物的区域选择性和化学选择性直接方法,该方法是通过在 Thf 中混合三异丁基铝 (Ibu3Al) 和四甲基哌啶锂 (Ltmp) 制备的,已经被开发出来.使用 Ibu3Al(Tmp)Li 对各种官能化苯进行去质子铝化,证明可有效直接生成各种邻位官能化铝芳香族和杂芳香族衍生物,尤其是具有亲电子官能团(如氰基,酰胺和卤素)的那些.直接铝化,然后进行亲电捕获(使用 I2),为 1,2-或 1,2,3-多取代芳族化合物提供了一种方便的制备方法.
Doi:10.1021/ja0473236

专利信息

专利号:US-6528642-B1
优先权日:1997-08-29
标题:Mono-and di-derivatives of cyclodextrins, synthesis thereof and purification and use thereof in support
发明人：DUVAL RAPHAEL; LEVEQUE HUBERT
权利人:INST FRANCAIS DU PETROLE; CHIRALSEP SARL
摘要:Mono- and di-derivatives of cyclodextrins are completely defined, also a method for their synthesis and purification, functionalised cyclodextrins obtained from these derivatives, and the synthesis of supports comprising these cyclodextrin derivatives. Use of the supports for the preparation or separation of enantiomers, for asymmetric synthesis, for catalysis, for the preparation or separation of geometrical isomers or positional isomers, or for the preparation or separation of organic molecules with a hydrophobic nature is also described.

专利号:US-6048991-A
优先权日:1990-11-16
标题:Preparation of epoxides
发明人：HAERMELING DIETER
权利人:BASF AG
摘要:Alpha-hydroxy-epoxides of alpha-alkoxy-epoxides of the formula IV ##STR1## in which the substituents have the following meanings: R 7 , R 8 , R 9 , R 10 , R 11 are independently hydrogen, C 1 -C 20 -alkyl, C 3 -C 12 -cycloalkyl, C 4 -C 20 -cycloalkylalkyl, C 1 -C 20 -hydroxy-alkyl, a heterocyclic ring, or an aryl or C 7 -C 20 -arylalkyl group optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen, C 1 -C 4 -haloalkyl, C 1 -C 4 -halo-alkoxy, phenyl, phenoxy, halophenyl, halophenoxy, carboxy, C 2 -C 8 -alkoxycarbonyl, or cyano, or R 7 and R 8 or R 7 and R 9 or R 7 and R 10 or R 9 and R 10 or R 10 and R 11 together form a (CH 2 ) n group in which n is an integer from 1 to 10 and which may be optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, and/or halogen, and n R 12 is hydrogen, C 1 -C 8 -alkyl, or benzyl, n provided that R 10 is not hydrogen, methyl, ethyl, propyl, or cyclohexyl when R 7 , R 8 , R 9 , or R 11 is hydrogen, that R 7 is not methyl when R 8 is methyl or phenyl and R 9 , R 10 , or R 11 is hydrogen, that R 7 is not methyl when R 8 , R 9 , R 10 , or R 11 is hydrogen and R 12 is ethyl, that R 7 is not phenyl or hexyl when R 8 , R 9 , R 10 , or R 11 is hydrogen, that R 9 is not methyl when R 7 , R 8 , R 10 , or R 11 is hydrogen, that R 10 and R 11 are not methyl when R 7 , R 8 , or R 9 is hydrogen, and that R 7 and R 10 do not together form an unsubstituted cycloalkyl when R 8 , R 9 , or R 11 is hydrogen. The epoxides of the above formula serve as intermediates for the synthesis of, inter alia, perfumes, plant protectants and polymers.

专利号:WO-2004087679-A1
优先权日:2003-04-01
标 题 :2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases
发明人：OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX
权利人:APONETICS AG; OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX
摘要:The invention relates to substituted pyrimidines of formula (I) wherein V represents a bond or CR6R7, W represents a bond, NR8 or oxygen, X represents sulfur, or nitrogen substituted by hydrogen or R5, Y represents -CH2-, -CH2CH2-, -CO- or -CS-, R1 represents unsubstituted or substituted aryl or heteroaryl, and the substituents R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification. These compounds are selectively inducing apoptosis in cancer cells and can be used for the treatment of neoplastic and autoimmune diseases. The invention relates also to methods of synthesis of such compounds, to their use as medicaments, to pharmaceutical compositions containing same, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.

专利号:US-10081610-B2
优先权日:2014-09-12
标题 :Efficient and scalable synthesis of 2-(1′h-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester and its structural analogs
发明人：SONG JIASHENG; ZHANG SUOMING; LI GUODONG; YANG LUQUING
权利人:ARIAGEN INC
摘要:Methods of synthesizing 2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) and structural analogs thereof. The methods include condensation reactions or condensation and oxidation reactions to form the thiazoline or thiazole moiety of ITE or its structural analogs.

专利号:US-4388310-A
优先权日:1982-03-01
标 题:6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids
发明人：CHRISTENSEN BURTON G; DININNO FRANK P; MUTHARD DAVID A; RATCLIFFE RONALD W
权利人:MERCK & CO INC
摘要:Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: I wherein: R1 is H or acyl; R2 is hydrogen or methoxyl; R3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.

专利号:US-10385010-B1
优先权日:2018-03-28
标 题 :Expedient synthesis of oseltamivir and related compounds via direct olefin diazidation-diamidation reaction
发明人：XU HAO; LI HONGZE; SHEN SHOUJIE; ZHU CHENGLIANG
权利人:UNIV GEORGIA STATE RES FOUND
摘要:Disclosed herein are improved methods for the preparation of oseltamivir, and intermediates useful thereto.