公开(公告)号：US4611058A

公开(公告)日：1986-09-09

申请号：US734362

申请日：1985-05-14

申请人： Wolfgang Koebernick

发明人： Wolfgang Koebernick

IPC分类号： C07B61/00 ,  C07D211/46

CPC分类号： C07D211/46

摘要： The invention relates to a process for preparing 1,5-didesoxy-1,5-imino-D-glucitol (desoxynojirimicin) and N-derivative thereof, which are known to be powerful inhibitors for .alpha.-glycosidases. The process of the invention involves reducing with a complex borohydride, a 6-amino-6-desoxy-L-sorbose.

摘要翻译： 本发明涉及制备1,5-二氧杂-1,5-亚氨基-D-葡萄糖醇（脱氧野尻霉素）及其N-衍生物的方法，其已知是α-糖苷酶的强大抑制剂。 本发明的方法包括用复合硼氢化物还原6-氨基-6-脱氧-L-山梨糖。

公开(公告)号：US4600778A

公开(公告)日：1986-07-15

申请号：US591614

申请日：1984-03-20

申请人： Werner Teller ,  Wolfgang Koebernick ,  Arthur Haaf ,  Paul Naab ,  Michael Preiss

发明人： Werner Teller ,  Wolfgang Koebernick ,  Arthur Haaf ,  Paul Naab ,  Michael Preiss

IPC分类号： C07C205/56 ,  C07D211/90 ,  C07B53/00

CPC分类号： C07C201/12 ,  C07D211/90

摘要： In the preparation of a 1,4-dihydropyridine of the formula ##STR1## in which R is a phenyl radical which is optionally substituted once or twice by nitro and/or chlorine,R.sub.1 is a C.sub.1 -C.sub.4 -alkyl radical which is optionally substituted by a C.sub.1 -C.sub.4 -alkoxy group, andR.sub.2 is a C.sub.1 -C.sub.12 -alkyl radical which is optionally substituted by a C.sub.1 -C.sub.4 -alkoxy group, a trifluoromethyl group or the radical (C.sub.6 H.sub.5 CH.sub.2) (CH.sub.3)N,by preparing an ylidene compound of the formula ##STR2## and reacting such ylidene compound with an enamine compound of the formula ##STR3## the improvement which comprises preparing the ylidene compound by reaction of a ketocarboxylic ester of the formula ##STR4## with an aldehyde of the formula RCHO, in a solvent in the presence of a catalytic amount of any acetate salt of an amine, at a temperature from about -10.degree. C. up to 100.degree. C. The products symmetrical or unsymmetrical, are produced in high yield and purity.

摘要翻译： 在制备式“IMAGE”的1,4-二氢吡啶的制备中，其中R是任选被硝基和/或氯取代一次或两次的苯基，R 1是任选取代的C 1 -C 4 - 烷基 通过C 1 -C 4 - 烷氧基，并且R 2是任选地被C 1 -C 4 - 烷氧基，三氟甲基或基团（C 6 H 5 CH 2）（CH 3）N）取代的C 1 -C 12 - 烷基， 并且使该亚基化合物与式“IMAGE”或“IMAGE”的烯胺化合物反应，该改进包括通过下式的酮羧酸酯反应制备亚基化合物： 或“IMAGE”与式RCHO的醛在溶剂中，在催化量的任何乙酸盐的存在下，在约-10℃至100℃的温度下进行。产物对称或 不对称，以高产率和纯度生产。

公开(公告)号：US4429117A

公开(公告)日：1984-01-31

申请号：US180778

申请日：1980-08-25

申请人： Wolfgang Koebernick ,  Hans-Rolf Furtwangler

发明人： Wolfgang Koebernick ,  Hans-Rolf Furtwangler

IPC分类号： C07H9/04 ,  C07H15/12 ,  C07H17/04

CPC分类号： C07H9/04 ,  C07H15/12

摘要： The invention relates, inter alia, to a process for the provision of 6-amino-6-desoxy-2,3-O-isopropylidene-.alpha.-L-sorbofuranose derivatives which comprises treating a 2,3-O-isopropylidene-6-sulphonated-.alpha.-L-sorbofuranase with an amine in an aqueous medium in an autoclave, followed by reaction of the reactions product in a basic medium to provide the free amine of Formula I as described hereinafter. The invention also includes the products obtained by the reaction and the invention further includes the process for providing the compounds of Formula VII as described hereinafter by treatment of a compound of Formula I as described hereinafter with an acid, followed by hydrogenation. The products of the invention are useful as medicaments or intermediates for medicaments.

摘要翻译： 本发明尤其涉及提供6-氨基-6-脱氧-2,3-O-异丙叉-α-L-呋喃核糖衍生物的方法，该方法包括处理2,3-O-异亚丙基-6- 在高压釜中的含水介质中加入磺化-α-L-呋喃并呋喃并与胺反应，随后将反应产物在碱性介质中反应，得到如下文所述的式I的游离胺。 本发明还包括通过反应和本发明获得的产物还包括如下所述通过用酸处理如下所述的式I化合物，随后氢化而提供如下所述的式VII化合物的方法。 本发明的产品可用作药物的药物或中间体。

公开(公告)号：US4405714A

公开(公告)日：1983-09-20

申请号：US305656

申请日：1981-09-25

申请人： Gunther Kinast ,  Michael Schedel ,  Wolfgang Koebernick

发明人： Gunther Kinast ,  Michael Schedel ,  Wolfgang Koebernick

IPC分类号： C12P19/02 ,  C07C67/00 ,  C07C213/00 ,  C07C215/10 ,  C07C225/06 ,  C07C271/16 ,  C07D211/46 ,  C07H5/06 ,  C07H15/12 ,  C07H15/18 ,  C12P19/26 ,  C12R1/01 ,  C12R1/15

CPC分类号： C12P19/26 ,  C07C271/16 ,  C07D211/46 ,  Y02P20/55

摘要： A process has been developed for the preparation of compounds of the formula ##STR1## wherein R is hydrogen or an optionally substituted alkyl radical, which comprises reacting glucose with a compound of the formula H.sub.2 N-R wherein R has the meaning given above to form a 1-amino-sorbitol of the formula ##STR2## wherein R has the meaning given above,reacting said 1-aminosorbitol with a compound providing a protective group which can be split off under acid conditions and is stable in the subsequent microbiological oxidation process, aerobically oxidizing the compound thus obtained microbiologically to give a protected 6-aminosorbose, splitting off the protective group under acid conditions and hydrogenating the 6-aminosorbose salt thus obtained either after being isolated or in one operation, to give the compound of the formula (I). The products obtained by the process of the invention are useful as .alpha.-glucoside inhibitors.

摘要翻译： 已经开发了制备式（I）化合物的方法，其中R是氢或任选取代的烷基，其包括使葡萄糖与式H2N-R化合物反应，其中R具有上述含义 以形成式（IV）的1-氨基 - 山梨糖醇，其中R具有上述含义，使所述1-氨基异山梨醇与提供保护基团的化合物反应，所述保护基团可在酸性条件下分离，并且在 随后的微生物氧化过程，对微生物获得的化合物进行有氧氧化，得到受保护的6-氨基异摩尔糖，在酸性条件下分离保护基团，并在分离或一次操作后氢化得到的6-氨基吗啡吗啡，得到化合物 的式（I）。 通过本发明方法获得的产物可用作α-葡萄糖苷抑制剂。

公开(公告)号：US4380625A

公开(公告)日：1983-04-19

申请号：US220640

申请日：1980-12-29

申请人： Peter Stadler ,  Wolfgang Koebernick ,  Samir Samaan ,  Wolfgang Gau

发明人： Peter Stadler ,  Wolfgang Koebernick ,  Samir Samaan ,  Wolfgang Gau

IPC分类号： C07H15/234 ,  C07H15/236 ,  C07H15/22

CPC分类号： C07H15/234

摘要： The invention relates to an improved process for the isolation and purification of aminoglycoside antibiotics of Formula (I) as defined herein combining selective lipophilization of the compound of Formula (I) in the crude product obtained by fermentation with controlled liquid/liquid extraction.

摘要翻译： 本发明涉及一种用于分离和纯化本发明定义的式（I）的氨基糖苷类抗生素的改进方法，该方法结合了通过用受控液/液萃取发酵获得的粗产物中式（I）化合物的选择性亲油化。