公开(公告)号：US4297519A

公开(公告)日：1981-10-27

申请号：US125617

申请日：1980-02-28

申请人： Werner Ertel

发明人： Werner Ertel

IPC分类号： C07C205/44 ,  C07C45/28 ,  C07C47/54 ,  C07C67/00 ,  C07C201/00

CPC分类号： C07C201/12 ,  C07C201/16

摘要： A process provided for the production of 2-nitrobenzaldehyde from 2-nitrotoluene, in which 2-nitrotoluene is converted, by bromination by a radical mechanism, to 2-nitrobenzyl bromide in the form of a bromination oil containing 20 to 50% or more of 2-nitrobenzyl bromide, and the bromination oil is oxidized directly with a mixture of dimethylsulphoxide and sodium bicarbonate in a weight ratio of 3:1 to 10:1 at temperatures of up to 100.degree. C. and the 2-nitrobenzaldehyde is subsequently isolated via the bisulphite adduct, to give 2-nitrobenzaldehyde in high purity and high yield. The process also has the advantage of a very short reaction time. The 2-nitrobenzaldehyde produced is an important intermediate, for example in the production of pharmaceutically active 1,4-dihydropyridines.

摘要翻译： 通过自由基机理的溴化将2-硝基甲苯转化为2-硝基甲苯的2-硝基苯甲醛制备为含有20〜50％以上的溴化油形式的2-硝基苄基溴的方法， 2-硝基苄基溴，溴化油直接用二甲基亚砜和碳酸氢钠的混合物以3:1至10:1的重量比在高达100℃的温度下氧化，然后将2-硝基苯甲醛通过 亚硫酸氢盐加合物，得到2-硝基苯甲醛，纯度高，产率高。 该方法还具有非常短的反应时间的优点。 产生的2-硝基苯甲醛是重要的中间体，例如在制备药物活性的1,4-二氢吡啶中。

公开(公告)号：US4229349A

公开(公告)日：1980-10-21

申请号：US27539

申请日：1979-04-05

申请人： Werner Ertel

发明人： Werner Ertel

IPC分类号： C07D233/38 ,  C07D499/00 ,  C07D499/12 ,  C07D499/68 ,  C07D501/06

CPC分类号： C07D233/38 ,  C07D499/00

摘要： In the production of a semi-synthetic .beta.-lactam antibiotic by reacting an amino compound of the formula ##STR1## in which X is the remaining members of a ring of a .beta.-lactam antibiotic, andR is a hydrogen atom or a methoxy group,with an activated carboxylic acid derivative of the formula ##STR2## in which R.sub.1 is an organic radical,B is an optionally substituted phenyl, cyclohexadienyl or heterocyclyl radical andR.sub.2 is a lower alkyl radical,the improvement which comprises effecting the reaction in an acetone/water mixture which contains acetone and water in a volume ratio of about 0.5:1 to 3:1. Advantageously the reaction is carried out at about -10.degree. to +10.degree. C. in the presence of an organic base employing about 1.1 to 1.2 mols of the amino compound per mol of the activated carboxylic acid derivative.

摘要翻译： 在通过使式“IMAGE”的氨基化合物与其中X是β-内酰胺抗生素的环的剩余成员反应而制备半合成β-内酰胺抗生素的方法中，R是氢原子或甲氧基 ，其中R1为有机基团的式为“IMAGE”的活化羧酸衍生物，B为任选取代的苯基，环己二烯基或杂环基，R2为低级烷基，其改进包括在丙酮中进行反应 /水混合物，其含有体积比为约0.5:1至3:1的丙酮和水。 有利地，在有机碱的存在下，在约-10℃至+ 10℃下进行反应，每摩尔活化的羧酸衍生物使用约1.1至1.2摩尔的氨基化合物。