公开(公告)号：US5204465A

公开(公告)日：1993-04-20

申请号：US803067

申请日：1991-12-06

申请人： David L. Kuo ,  Robert Voeffray

发明人： David L. Kuo ,  Robert Voeffray

IPC分类号： C07D239/42

CPC分类号： C07D239/42

摘要： A process for the production of piperazinylpyrimidine derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, branched or unbranched. These piperazinylpyrimidine derivatives are acid-converted with cyanamide to an amidine salt starting from piperazine or its hydrate and then reacted with a dicarbonyl compound in the presence of a base to the end product.

摘要翻译： 制备下式的哌嗪基嘧啶衍生物的方法：其中R 1，R 2和R 3相同或不同，并且各自为氢原子或支链或非支链的C 1 -C 4烷基。 这些哌嗪基嘧啶衍生物用氨基氰酸转化为脒盐，从哌嗪或其水合物开始，然后与二羰基化合物在碱存在下与最终产物反应。

公开(公告)号：US5498715A

公开(公告)日：1996-03-12

申请号：US350083

申请日：1994-11-29

申请人： David L. Kuo ,  Martin Eyer ,  Jean-Paul Roduit ,  Alain Wellig

发明人： David L. Kuo ,  Martin Eyer ,  Jean-Paul Roduit ,  Alain Wellig

IPC分类号： B01J31/04 ,  C07B61/00 ,  C07D471/04

CPC分类号： C07D471/04

摘要： A process for preparing imidazopyridine derivatives of the general formula: ##STR1## wherein R.sub.1 is hydrogen or an alkyl group, and R.sub.2, R.sub.3 and R.sub.4 are identical or different and are hydrogen, an alkyl group, a cycloalkyl group, an aryl group, an aralkyl group or a halogen atom. In this process, a 2-amino-3-nitropyridine is hydrogenated in the presence of a hydrogenation catalyst and the hydrogenation product is condensed with a carboxylic acid simultaneously present in the reaction mixture to give the end product. The imidazopyridine derivatives are intermediates for the preparation of angiotensin II antagonists.

摘要翻译： 制备通式如下的咪唑并吡啶衍生物的方法：其中R 1是氢或烷基，R 2，R 3和R 4相同或不同并且是氢，烷基，环烷基，芳基， 芳烷基或卤素原子。 在该方法中，2-氨基-3-硝基吡啶在氢化催化剂存在下氢化，氢化产物与同时存在于反应混合物中的羧酸缩合得到最终产物。 咪唑并吡啶衍生物是制备血管紧张素II拮抗剂的中间体。

公开(公告)号：US5200520A

公开(公告)日：1993-04-06

申请号：US804372

申请日：1991-12-10

申请人： David L. Kuo

发明人： David L. Kuo

IPC分类号： C07D239/42

CPC分类号： C07D239/42

摘要： A process for the production of piperazinylpyrimidine derivatives of the formula I: ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, branched or unbranched. In the process, piperazine or its hydrate is acid-converted with cyanamide to an amidine salt and the latter is then reacted with a carbonyl compound in the presence of a base to the end product.

摘要翻译： 制备式I的哌嗪基嘧啶衍生物的方法：其中R 1是氢原子或C 1 -C 4烷基，是支链或非支链的。 在此过程中，将哌嗪或其水合物用氰胺酸转化为脒盐，然后将其与羰基化合物在碱的存在下与最终产物反应。

公开(公告)号：US5919992A

公开(公告)日：1999-07-06

申请号：US661671

申请日：1996-06-11

申请人： David L. Kuo

发明人： David L. Kuo

IPC分类号： C07C31/34 ,  C07C29/62 ,  C07C33/04 ,  C07C33/42

CPC分类号： C07C29/62

摘要： The present invention relates to process of halogenating an alkynol having 3 to 20 carbon atoms to produce a compound having the formula: R-C.tbd.(C--CH.sub.2).sbsb.x-OH, wherein R is F, Cl, Br or I and x is 1 to 18. In particular, this invention provides a process for preparing a halopropynyl alcohol, specifically iodopropynyl alcohol. In one embodiment, iodopropynyl alcohol is produced by sequentially adding potassium hydroxide, potassium iodide and an oxidizing agent to a solution of propynyl alcohol at a rate and temperature sufficient to produce an iodopropynyl alcohol.

摘要翻译： 本发明涉及卤化具有3至20个碳原子的炔醇的方法，以制备具有下式的化合物：RC 3BOND（C-CH 2）x -OH，其中R为F，Cl，Br或I，x为1至 特别地，本发明提供了制备卤代丙炔醇，特别是碘丙炔醇的方法。 在一个实施方案中，碘丙炔醇通过以足以产生碘丙炔醇的速率和温度依次加入氢氧化钾，碘化钾和氧化剂来制备。

公开(公告)号：US20120226044A1

公开(公告)日：2012-09-06

申请号：US11630562

申请日：2005-07-04

申请人： Yves Bessard ,  David L. Kuo

发明人： Yves Bessard ,  David L. Kuo

IPC分类号： C07D221/18

CPC分类号： C07J73/005

摘要： A process for the preparation of 4-steroids of the formula: R1 and R2 are independently selected from the group that is hydrogen, F, Cl, Br, I, C1-6-allyl and C1-6-alkoxy, and R4 is selected from the group that is hydrogen, (N,N-di-C1-6-allylamino)methyl, allylamino)ethyl, C1-6-alkyl, C1-6-alkoxy, phenyl and benzyl, and Q7 represents a carbonyl oxygen atom or is R7-1 and R7-2, wherein one of R7-1 and R7-2 is hydrogen and the other is selected from the group that is hydrogen, F, Cl, Br, I, C1-6-alkyl and C1-6-alkoxy, and R9 represents hydrogen or F, and Q11 represents a carbonyl oxygen atom or is R11-1 and R11-2, wherein one of R11-1 and R11-2 is hydrogen and the other is selected from the group that is hydrogen, cyano, cyano-C1-3-alkyl, acetoxy, COOH and COO−M+, wherein M+ is Na+, K+ or NH+4, and R16 is selected from the group that is hydrogen, cyano, cyano-C1-3-alkyl, acetoxy, COOH and COO−M+, wherein M+ is Na+, K+ or NH+4, and COOR represents COOH or COO−M+, wherein M+ is Na+, K+ or NH+4. The three step process includes (i) a haloform reaction of a 17-acetyl steroid converting the acetyl group into a —COOR group, (ii) subsequent ozonolysis of the A-ring and (iii) reclosure of the A-ring by reaction with an appropriate nitrogen compound of formula H2NR4 to afford a compound of formula I above.

摘要翻译： 用于制备下式的4-类固醇的方法：R 1和R 2独立地选自氢，F，Cl，Br，I，C 1-6 - 烯丙基和C 1-6 - 烷氧基，并且选择R 4 （N，N-二-C 1-6烯丙基氨基）甲基，烯丙基氨基）乙基，C 1-6 - 烷基，C 1-6 - 烷氧基，苯基和苄基，Q 7表示羰基氧原子或 是R7-1和R7-2，其中R7-1和R7-2之一是氢，另一个选自氢，F，Cl，Br，I，C 1-6 - 烷基和C 1-6的基团 - 烷氧基，R 9表示氢或F，Q 11表示羰基氧原子，或者是R 11-1和R 11-2，其中R 11-1和R 11-2中的一个是氢，另一个选自氢 ，氰基，氰基-C 1-3 - 烷基，乙酰氧基，COOH和COO-M +，其中M +是Na +，K +或NH + 4，R 16选自氢，氰基，氰基-C 1-3 - ，乙酰氧基，COOH和COO-M +，其中M +是Na +，K +或NH + 4，COOR表示COOH或COO-M +，其中M +是Na + K +或NH + 4。 三步法包括（i）将乙酰基转化为-COOR基团的17-乙酰基类固醇的卤代甲酰化反应，（ii）A环随后的臭氧分解和（iii）通过与 合适的式H2NR4的氮化合物，得到上述式I的化合物。

公开(公告)号：US5221748A

公开(公告)日：1993-06-22

申请号：US668116

申请日：1991-03-12

申请人： David L. Kuo

发明人： David L. Kuo

IPC分类号： B01J27/122 ,  B01J27/22 ,  C07B61/00 ,  C07D213/61

CPC分类号： C07D213/61

摘要： Process for the production of 2,3-dichloro-5-acetylpyridine by reaction of a 5,6-dichloronicotinic acid halide with a methyl magnesium halide in an inert organic diluent. The reaction is performed in the presence of a Cu/Cu halide as the catalyst.

摘要翻译： 通过5,6-二氯烟酰卤与甲基卤化镁在惰性有机稀释剂中的反应制备2,3-二氯-5-乙酰基吡啶的方法。 反应在Cu / Cu卤化物作催化剂存在下进行。