公开(公告)号：US4145437A

公开(公告)日：1979-03-20

申请号：US845420

申请日：1977-10-25

申请人： David C. Aldridge ,  Graham C. Crawley ,  Colin J. Strawson

发明人： David C. Aldridge ,  Graham C. Crawley ,  Colin J. Strawson

IPC分类号： C07C59/285 ,  C07D307/33 ,  C07D307/32 ,  A61K31/365

CPC分类号： C07D307/33 ,  C07C59/285

摘要： The invention concerns novel racemic and optically active mono- and di-hydroxy alkanoic acids bearing phenyl and/or alkyl substituents, processes for their preparation, and pharmaceutical compositions for therapeutic use in the treatment of duodenal or gastric ulcers. Representative compounds of the invention are 2-(5.beta.-n-butyl-4.beta.-hydroxy-2-oxo-tetrahydrofuran-3.beta.-yl)-2.alpha.-methyl-acetic acid and 3.alpha.-methyl-5.beta.-(1.beta.-hydroxy-n-pentyl)-2-oxo-tetrahydrofuran-4.beta.-ylcarboxylic acid.

公开(公告)号：US4178213A

公开(公告)日：1979-12-11

申请号：US864473

申请日：1977-12-27

申请人： David C. Aldridge ,  Roger Bowling ,  John C. Swait

发明人： David C. Aldridge ,  Roger Bowling ,  John C. Swait

IPC分类号： C07D307/33 ,  C12P17/04 ,  C12D13/00

CPC分类号： C07D307/33 ,  C12P17/04 ,  Y10S435/933

摘要： The invention concerns a fermentation process for the production of (+)-2-(5.beta.-n-butyl-4.beta.-hydroxy-2-oxo-tetrahydrofuran-3.beta.-yl)-2.alpha.-methylacetic acid, which compound has useful ulcer-healing properties. The process is characterised by cultivating an organism known to produce dihydrocanadensolide, such as Penicillium canadense, under generally conventional conditions and then extracting the culture filtrate at a pH in the range pH 3.0-7.0 with a suitable solvent, such as ethyl acetate, and then evaporating the extract to dryness. In a preferred embodiment the extraction is carried out on the culture filtrate at pH 4.0-4.5.

摘要翻译： 本发明涉及产生（+） - 2-（5β-正丁基-4β-羟基-2-氧代 - 四氢呋喃-3β-基）-2α-甲基乙酸的发酵方法，该化合物具有 有用的溃疡愈合属性。 该方法的特征在于在一般常规条件下培养已知生产二氢甘油多异丙二醇（例如青霉菌）的生物，然后用合适的溶剂如乙酸乙酯在pH3.0-7.0的pH范围内提取培养滤液，然后 将提取物蒸发至干燥。 在优选的实施方案中，在pH 4.0-4.5的培养滤液上进行萃取。