公开(公告)号：US4716237A

公开(公告)日：1987-12-29

申请号：US475395

申请日：1983-03-15

Applicant: Karlheinz Drauz ,  Axel Kleemann ,  Elisabeth Wolf-Heuss

Inventor： Karlheinz Drauz ,  Axel Kleemann ,  Elisabeth Wolf-Heuss

IPC: A01N43/08 ,  C07C67/00 ,  C07C253/00 ,  C07C255/17 ,  C07C255/31 ,  C07C255/32 ,  C07C255/40 ,  C07C255/45 ,  C07C255/56 ,  C07D307/54 ,  C07D307/68 ,  C07D333/24 ,  C07D333/38 ,  C07C121/34 ,  C07C121/76

CPC classification number: C07C255/00 ,  C07C253/30 ,  C07D307/54 ,  C07D333/24

Abstract: 3-oxonitriles are produced by reaction of carboxylic acid esters with carboxylic acid nitriles in the presence of 70 to 80% suspension of sodium hydride in white oil. The oxonitrile are intermediate products for the production of 3-oxocarboxylic acid amides or esters and pesticides.

公开(公告)号：US4618730A

公开(公告)日：1986-10-21

申请号：US587652

申请日：1984-03-08

Applicant: Karlheinz Drauz ,  Axel Kleemann

Inventor： Karlheinz Drauz ,  Axel Kleemann

IPC: C07C27/00 ,  C07C37/60 ,  C07C39/08 ,  C07C67/00 ,  C07C39/10

CPC classification number: C07C37/60 ,  Y02P20/582

Abstract: The known nuclear hydroxylation of phenol with organic solutions of hydrogen peroxide in the presence of a catalyst is carried out in improved manner by employing both (1) a special, practically water free solution of hydrogen peroxide in an organic solvent which forms an azeotrope with water, which azeotrope boils below the boiling point of hydrogen peroxide, and (2) sulfur dioxide as a catalyst. Through this, the nuclear hydroxylation is substantially simpler than previously; difficult separations, e.g., from water-phenol, or the separation and recovery of the catalyst are eliminated. Besides, the yields are increased.

Abstract translation: 在催化剂存在下，酚与有机过氧化物的已知核羟基化反应是通过使用（1）在与水形成共沸物的有机溶剂中的特殊的实际上无水的过氧化氢溶液来进行的 ，其共沸物沸点低于过氧化氢的沸点，和（2）二氧化硫作为催化剂。 通过这一点，核羟基化比以前简单得多; 难以分离，例如来自水 - 苯酚，或者分离和回收催化剂。 此外，收益率上升。

公开(公告)号：US4602096A

公开(公告)日：1986-07-22

申请号：US764993

申请日：1985-08-12

Applicant: Michael Karrenbauer ,  Axel Kleemann

Inventor： Michael Karrenbauer ,  Axel Kleemann

IPC: C07C313/00 ,  C07B55/00 ,  C07C67/00 ,  C07C227/36 ,  C07C231/12 ,  C07C233/47 ,  C07C319/20 ,  C07C323/59 ,  C07D209/20

CPC classification number: C07D209/20

Abstract: N-acetyl-D(L)-.alpha.-aminocarboxylic acids are thermally racemized by melting, adding a small amount of acetic anhydride to the melt and heating to a temperature between the melting temperature and about 210.degree. C. and subsequently quenching the melt with an aqueous alkali metal hydroxide or ammonia solution. The residence time needed for complete racemization depends on the heating temperature of the melt in the manner that the higher the heating temperature the shorter the residence time.

Abstract translation: N-乙酰基-D（L）-α-氨基羧酸通过熔融进行外消旋化，向熔体中加入少量乙酸酐并加热到熔融温度至约210℃之间的温度，随后用 碱金属氢氧化物水溶液或氨水溶液。 完全外消旋化所需的停留时间取决于熔体的加热温度，其方式是加热温度越高停留时间越短。

公开(公告)号：US4550200A

公开(公告)日：1985-10-29

申请号：US590059

申请日：1984-03-15

Applicant: Michael Karrenbauer ,  Axel Kleemann ,  Theodor Lussling ,  Fritz Schafer

Inventor： Michael Karrenbauer ,  Axel Kleemann ,  Theodor Lussling ,  Fritz Schafer

IPC: C07C319/24 ,  C07C67/00 ,  C07C313/00 ,  C07C323/58 ,  C07C149/243

CPC classification number: C07C319/12

Abstract: D,L-Homocystine is obtained by introducing molecular oxygen into an aqueous solution of the disodium salt of D,L-homocysteine having a concentration between 0.8 and 1.2 moles/l and an initial pH between 7.0 and 8.0 in the presence of a catalytic amount of iron(III) ions until there is no longer an increase in pH and subsequently adjusting the pH to about 5.3 with stirring.

Abstract translation: 通过将分子氧引入浓度在0.8和1.2摩尔/升之间的D，L-高半胱氨酸的二钠盐水溶液中，并且在催化量存在下将初始pH值介于7.0和8.0之间，得到D，L-高等胱氨酸 的铁（III）离子，直到pH不再增加，随后在搅拌下将pH调节至约5.3。

公开(公告)号：US4533766A

公开(公告)日：1985-08-06

申请号：US587654

申请日：1984-03-08

Applicant: Karlheinz Drauz ,  Axel Kleemann

Inventor： Karlheinz Drauz ,  Axel Kleemann

IPC: C07C43/23 ,  C07C27/00 ,  C07C37/60 ,  C07C39/08 ,  C07C41/00 ,  C07C41/26 ,  C07C67/00 ,  C07C37/00

CPC classification number: C07C37/60 ,  C07C41/26 ,  Y02P20/582

Abstract: The known nuclear hydroxylation of substituted phenols or phenol ethers with organic solutions of hydrogen peroxide in the presence of a catalyst is carried out in improved manner by employing both (1) a special, practically water free solution of hydrogen peroxide in an organic solvent which forms an azeotrope with water, which azeotrope boils below the boiling point of hydrogen peroxide, and (2) sulfur dioxide as a catalyst. Through this, the nuclear hydroxylation is substantially simpler than previously; difficult separations, e.g., from water-phenol, or the separation and recovery of the catalyst are eliminated. Besides, the yields are increased.

Abstract translation: 在催化剂存在下，用有机过氧化氢溶液对已取代的酚或苯酚醚进行已知的核羟基化反应是通过使用（1）特殊的实际上无水的过氧化氢溶液在有机溶剂中形成的 与水共沸，共沸物沸点低于过氧化氢的沸点，和（2）二氧化硫作为催化剂。 通过这一点，核羟基化比以前简单得多; 难以分离，例如来自水 - 苯酚，或者分离和回收催化剂。 此外，收益率上升。

公开(公告)号：US4469876A

公开(公告)日：1984-09-04

申请号：US418841

申请日：1982-09-16

Applicant: Karlheinz Drauz ,  Axel Kleemann ,  Jurgen Martens ,  Paul Scherberich ,  Franz Effenberger

Inventor： Karlheinz Drauz ,  Axel Kleemann ,  Jurgen Martens ,  Paul Scherberich ,  Franz Effenberger

IPC: C07D207/16 ,  C07D207/22 ,  C07D207/12

CPC classification number: C07D207/16 ,  C07D207/22

Abstract: L-proline is produced from the methyl or ethyl ester of L-pyroglutamic acid by reacting this with at least twice the molar amount of phosgene to form the corresponding 1-chlorocarbonyl-5,5-dichloroproline ester, producing the corresponding 2-chloro-1-chlorocarbonyl-pyrrolin-(2)-carboxylic acid ester-(5) therefrom by splitting off hydrogen chloride, catalytically hydrogenating the pyrrolin-(2) compound to the corresponding N-chlorocarbonyl-proline ester and hydrolyzing the latter with acid to form L-proline.

Abstract translation: 通过将其与至少两倍摩尔量的光气反应形成相应的1-氯羰基-5,5-二氯脯氨酸酯，由L-焦谷氨酸的甲酯或乙酯制备L-脯氨酸，产生相应的2-氯 - 通过分离氯化氢，将吡咯啉 - （2）化合物催化氢化成相应的N-氯羰基 - 脯氨酸酯并用酸水解后者形成1-氯羰基 - 吡咯啉 - （2） - 羧酸酯 - （5） L-脯氨酸。

公开(公告)号：US4419272A

公开(公告)日：1983-12-06

申请号：US351404

申请日：1982-02-23

Applicant: Bergstein Wolfgang ,  Heinz Friedrich ,  Axel Kleemann ,  Gunther Prescher ,  Helmut Beschke

Inventor： Bergstein Wolfgang ,  Heinz Friedrich ,  Axel Kleemann ,  Gunther Prescher ,  Helmut Beschke

IPC: B01J21/16 ,  B01J23/22 ,  B01J23/34 ,  B01J23/84 ,  B01J35/10 ,  C07B61/00 ,  C07D241/24 ,  B01J23/16

CPC classification number: C07D241/24 ,  B01J21/16 ,  B01J23/22 ,  B01J23/34 ,  B01J23/84 ,  B01J35/10 ,  B01J35/1014 ,  B01J35/1038 ,  B01J35/1066 ,  B01J35/1071

Abstract: For the catalytic reaction of 2-methylpyrazine with ammonia and oxygen to form 2-cyanopyrazine there are used compounds of the elements antimony, vanadium, and oxygen and at least one of the elements iron, copper, titanium, cobalt, manganese, and nickel, whereby the atomic ratio of antimony to vanadium is greater than 1 and which contain besides these compounds a lattice layer silicate and a highly dispersed silica. These catalysts are very selective and result in high yields and high space-time-yields.

公开(公告)号：US4369322A

公开(公告)日：1983-01-18

申请号：US241836

申请日：1981-03-09

Applicant: Peter Schalke ,  Axel Kleemann

Inventor： Peter Schalke ,  Axel Kleemann

IPC: C07C255/00 ,  C07B31/00 ,  C07B43/08 ,  C07C67/00 ,  C07C253/00 ,  C07C255/32 ,  C07C255/33 ,  C07C255/36 ,  C07C255/37 ,  C07C255/53 ,  C07D213/57 ,  C07D213/61 ,  C07D213/84 ,  C07D333/24 ,  C07D333/38 ,  C07C120/00 ,  C07C121/66 ,  C07C121/68

CPC classification number: C07C253/04 ,  C07D213/57 ,  C07D333/24

Abstract: The known synthesis for the production of aromatic substituted acetonitriles by reaction of aromatic substances with cyanogen chloride in the gas phase is improved by feeding the starting materials in gaseous form and separated from each other into the reactor. The process can be used to synthesize in general aromatic and especially hetero-aromatic substituted acetonitrile.

Abstract translation: 芳族物质与氯化氰在气相中的反应生产芳族取代的乙腈的已知合成通过将原料以气态形式供入反应器而得到改善。 该方法可用于合成通常的芳族和特别是杂芳族取代的乙腈。

公开(公告)号：US4339591A

公开(公告)日：1982-07-13

申请号：US246313

申请日：1981-03-23

Applicant: Axel Kleemann ,  Bernd Lehmann ,  Herbert Klenk

Inventor： Axel Kleemann ,  Bernd Lehmann ,  Herbert Klenk

IPC: B01J31/00 ,  B01J31/02 ,  C07C20060101 ,  C07C67/00 ,  C07C253/00 ,  C07C255/02 ,  C07C255/31 ,  C07C255/45 ,  C07C255/56 ,  C07D307/54 ,  C07D333/24 ,  C07C120/04

CPC classification number: C07C253/14 ,  C07C2101/02

Abstract: There are produced carboxylic acid cyanides, e.g., acyl cyanides by reacting a carboxylic acid halide with an alkali cyanide or hydrogen cyanide in the presence of a copper (I) salt and a carboxylic acid nitrile. Especially advantageous are glutaric acid dinitrile and 2-methyl glutaric acid dinitrile.

Abstract translation: 通过羧酸卤化物与碱金属氰化物或氰化氢在铜（I）盐和羧酸腈的存在下反应，产生羧酸氰化物，例如酰基氰化物。 特别有利的是戊二酸二腈和2-甲基戊二酸二腈。

公开(公告)号：US4317832A

公开(公告)日：1982-03-02

申请号：US72777

申请日：1979-09-05

Applicant: Karl-Heinz Klingler ,  Axel Kleemann ,  Fritz Stroman ,  Klaus Thiemer

Inventor： Karl-Heinz Klingler ,  Axel Kleemann ,  Fritz Stroman ,  Klaus Thiemer

IPC: A61K31/155 ,  A61K31/403 ,  A61K31/405 ,  A61P25/02 ,  A61P27/02 ,  C07C67/00 ,  C07C239/00 ,  C07C279/04 ,  C07C279/12 ,  C07D209/08 ,  C07D209/43 ,  C07D209/86 ,  C07D209/88 ,  A61K31/40 ,  C07D209/14

CPC classification number: C07D209/08 ,  C07C279/12 ,  C07D209/88

Abstract: Compounds corresponding to the formula ##STR1## are disclosed, wherein Alk represents a C.sub.2 -C.sub.5 -alkylene groups optionally substituted by a hydroxy group and Ar represent an optionally substituted phenyl, naphthyl, tetrahydronaphthyl, indanyl or indenyl radical or a monocyclic or condensed bicyclic or tricyclic heterocyclic radical which is optionally substituted, the heterocyclic radical consisting of individual rings having 5 or 6 members and optionally containing from 1 to 4 hetero atoms, and the acid addition salts thereof. A process for producing these compounds is also disclosed. These substituted aminoalkyl guanidines block the .beta.-receptors of the adrenergic nerve system, and also reduce blood pressure.

Abstract translation: 公开了对应于式I的化合物，其中Alk表示任选被羟基取代的C 2 -C 5亚烷基，Ar表示任选取代的苯基，萘基，四氢萘基，茚满基或茚基或单环或稠合双环 或任选取代的三环杂环基，由具有5或6个成员且任选地含有1至4个杂原子的各个环组成的杂环基及其酸加成盐。 还公开了制备这些化合物的方法。 这些取代的氨基烷基胍可以阻断肾上腺素能神经系统的β受体，并降低血压。