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1. 发明申请

WO00008011A1 PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2-[6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL]ACETIC ACID DERIVATIVES 审中-公开
标题翻译：制备光学活性的2- [6-（羟基甲基）-1,3-二氧戊环-4-基]乙酸衍生物的方法
公开(公告)号：WO00008011A1
公开(公告)日：2000-02-17
申请号：PCT/JP1999/004229
申请日：1999-08-05
IPC分类号： C07C67/343 , C07C253/30 , C07C255/21 , C07D319/06 , C12P7/62 , C07C51/353 , C07C59/115 , C07C59/90 , C07D319/08 , C12P7/04
CPC分类号： C07D319/06 , C07B2200/07 , C07C67/343 , C07C253/30 , C12P7/62 , C07C69/716 , C07C255/21
摘要： A process for the preparation of optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which comprises subjecting an enolate prepared by reacting an acetate ester derivative with either a base or a zero-valent metal to reaction with a hydroxybutyric acid derivative at -30 DEG C or above to thereby obtain a hydroxyoxohexanoic acid derivative, reducing this hydroxyoxohexanoic acid derivative with a microorganism into a dihydroxyhexanoic acid derivative, treating this dihydroxyhexanoic acid derivative with an acetal-forming reactant in the presence of an acid to thereby obtain a halomethyldioxanylacetic acid derivative, acyloxylating this halomethyldioxanylacetic acid derivative with an acyloxylating agent into an acyloxymethyldioxanylacetic acid derivative, and subjecting this acyloxymethyldioxanylacetic acid derivative to solvolysis in the presence of a base.
摘要翻译：一种制备光学活性2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括使乙酸酯衍生物与碱或零在-30℃以上与羟基丁酸衍生物反应，得到羟基氧基己酸衍生物，用微生物将该羟基氧基己酸衍生物还原成二羟基己酸衍生物，用缩醛形成反应物处理该二羟基己酸衍生物在酸的存在下，得到卤代甲基二恶烷基乙酸衍生物，将该卤代甲基二恶烷基乙酸衍生物用酰氧基化剂酰化成酰氧基甲基二恶烷基乙酸衍生物，并使该酰氧基甲基二恶烷基乙酸衍生物在碱存在下溶剂解。

2. 发明申请

WO99032434A1 PROCESS FOR THE SYNTHESIS OF 1,3-DIOLS 审中-公开
标题翻译： 1,3-二醇合成方法
公开(公告)号：WO99032434A1
公开(公告)日：1999-07-01
申请号：PCT/US1998/025493
申请日：1998-12-02
IPC分类号： C07B31/00 , C07B41/02 , C07C29/143 , C07C253/30 , C07C255/20 , C07C255/21 , C07D207/34 , C07D207/40 , C07D207/416
CPC分类号： C07D207/416 , C07B41/02 , C07B2200/07 , C07C253/30 , C07C255/20 , C07C255/21 , C07D207/34 , Y02P20/55
摘要： An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.
摘要翻译：描述了制备顺式-1,3-二醇的改进方法，其中用三烷基硼烷或二烷基烷氧基硼烷或三烷基硼烷和二烷基烷氧基硼烷的混合物处理β-羟基酮，然后回收和再利用烷基硼烷物质以转化另外的β 羟基酮与顺式-1,3-二醇反应。

3. 发明申请

WO2011048425A1 CONTINUOUS PROCESS FOR THE PRODUCTION OF BETA-KETO ESTERS BY CLAISEN CONDENSATION 审中-公开
标题翻译：通过分散剂浓缩生产β-葡萄糖酸酯的连续方法
公开(公告)号：WO2011048425A1
公开(公告)日：2011-04-28
申请号：PCT/GB2010/051778
申请日：2010-10-22
申请人： PHOENIX CHEMICALS LIMITED , MCCORMACK, Peter , WARR, Antony, John , LATHAM, Elliot
发明人： MCCORMACK, Peter , WARR, Antony, John , LATHAM, Elliot
IPC分类号： C07C255/21 , C07C69/675 , C07C69/716 , C07C67/31 , C07C67/343 , C07D319/06
CPC分类号： C07C253/30 , C07C67/343 , C07D319/06 , C07C69/716 , C07C255/21
摘要： The invention concerns a continuous process for the production of compounds having the general formula (6) comprising providing to a reaction zone a continuous stream of an alkyl acetate and a continuous stream of an alkali metal or alkaline earth metal amide base and contacting the continuous streams together in the reaction zone to yield an enolate compound, providing to the or a separate reaction zone a continuous stream of a compound of formula (5) and contacting the continuous stream of compound (5) with a continuous stream of the enolate in the or the separate reaction zone at a temperature above 20°C to yield an intermediate compound and treating the intermediate compound of formula (1) with an acid to yield the compound of formula (6).
摘要翻译：本发明涉及用于生产具有通式（6）的化合物的连续方法，包括向反应区提供乙酸烷基酯和连续的碱金属或碱土金属酰胺碱基物流的连续流，并使连续流在反应区中一起产生烯醇化合物，向该或单独的反应区提供式（5）化合物的连续流，并将化合物（5）的连续流与连续的烯醇化合物流接触，在高于20℃的温度下分离反应区，得到中间体化合物，并用酸处理式（1）的中间体化合物，得到式（6）化合物。

4. 发明申请

WO2005026107A1 NOVEL PROCESS FOR THE PREPARATION OF TERT-BUTYL 6-CYANO-5-HYDROXY-3-OXOHEXANOATE 审中-公开
标题翻译：制备叔丁基6-氰基-5-羟基-3-氧代十六烷酸的新方法
公开(公告)号：WO2005026107A1
公开(公告)日：2005-03-24
申请号：PCT/IN2003/000317
申请日：2003-09-18
申请人： BIOCON LIMITED , SRINATH, Sumithra , PUTHIAPARAMPIL, Tom, Thomas , GANESH, Sambasivam
发明人： SRINATH, Sumithra , PUTHIAPARAMPIL, Tom, Thomas , GANESH, Sambasivam
IPC分类号： C07C255/23
CPC分类号： C07C253/30 , C07C255/21 , C07F7/1852
摘要： A novel process for preparation of tert -butyl 6-cyano-5-hydroxy-3-oxohexanoate, which is a key intermediate for the preparation of HMG COA reductase inhibitor, is disclosed.
摘要翻译：公开了制备HMG COA还原酶抑制剂的关键中间体6-氰基-5-羟基-3-氧代己酸叔丁酯的新方法。

5. 发明申请

WO00075099A1 PROCESSES FOR THE PREPARATION OF 5-HYDROXY-3-OXOPENTANOIC ACID DERIVATIVES 审中-公开
标题翻译：制备5-羟基-3-氧代戊酸衍生物的方法
公开(公告)号：WO00075099A1
公开(公告)日：2000-12-14
申请号：PCT/JP2000/003574
申请日：2000-06-02
IPC分类号： C07C67/343 , C07C253/30 , C07C255/21 , C07D319/06 , C12P7/62 , C07C69/716
CPC分类号： C12P7/62 , C07B2200/07 , C07C67/343 , C07C253/30 , C07D319/06 , C07C69/716 , C07C255/21 , C07C69/738
摘要： Processes by which 5-hydroxy-3-oxopentanoic acid derivatives useful as intermediates of drugs can be prepared from inexpensive and easily available raw materials under noncryogenic conditions. Specifically, a process for preparing 5-hydroxy-3-oxopentanoic acid derivatives by making lithium amide act on a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at a temperature of -20 DEG C or above; and another process for preparing 5-hydroxy-3-oxopentanoic acid derivatives by treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent and then making lithium amide act on the resulting mixture at a temperature of -20 DEG C or above.
摘要翻译：可用于药物中间体的5-羟基-3-氧代戊酸衍生物的方法可以在非高温条件下由廉价且容易获得的原料制备。具体而言，在-20℃以上的温度下，通过使氨基化锂作用于乙酸酯和3-羟基丙酸衍生物的混合物而制备5-羟基-3-氧代戊酸衍生物的方法; 以及通过用格氏试剂处理乙酸酯和3-羟基丙酸衍生物的混合物然后在-20℃的温度下使所得混合物起作用而制备5-羟基-3-氧代戊酸衍生物的另一种方法 ℃以上。

6. 发明申请

WO1996015096A1 SUBSTITUTED 4-BIARYLBUTYRIC OR 5-BIARYLPENTANOIC ACIDS AND DERIVATIVES AS MATRIX METALLOPROTEASE INHIBITIORS 审中-公开
标题翻译：作为基质金属蛋白酶抑制剂的取代的4-二异丁基或5-二氨基戊酸和衍生物
公开(公告)号：WO1996015096A1
公开(公告)日：1996-05-23
申请号：PCT/US1995014002
申请日：1995-11-09
申请人： BAYER CORPORATION , KLUENDER, Harold, Clinton, Eugene , BENZ, Guenter, Hans, Heinz, Herbert , BRITTELLI, David, Ross , BULLOCK, William, Harrison , COMBS, Kerry, Jeanne , DIXON, Brian, Richard , SCHNEIDER, Stephan , WOOD, Jill, Elizabeth , VANZANDT, Michael, Christopher , WOLANIN, Donald, John , WILHELM, Scott, M.
发明人： BAYER CORPORATION
IPC分类号： C07C59/88
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA-B-D-E-G, wherein A and B are aryl or heteroaryl rings; each T is a substituent group; x is 0, 1, or 2; the group D represents (a), (b), (c), (d), or (e); the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents -PO3H2, -M, (f), (g), or (h), in which M represents -CO2H, -CON(R )2, or -CO2R ; and R represents any of the side chains of the 19 noncyclic naturally occurring amino acids, and include pharmaceutically acceptable salts thereof.
摘要翻译：基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。本发明的化合物具有通式（T）xA-B-D-E-G，其中A和B是芳基或杂芳基环; 每个T是取代基; x为0,1或2; D组代表（a），（b），（c），（d）或（e）; 基团E表示一个或三个带有一个至三个独立的或参与环形成的取代基的碳链，可能的结构在本文和权利要求中示出; 并且基团G表示-PO 3 H 2，-M，（f），（g）或（h），其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12。并且R 13表示19个非环状天然存在的氨基酸的任何侧链，并且包括其药学上可接受的盐。

7. 发明申请

WO1996000570A1 ANTIBACTERIAL AGENT 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1996000570A1
公开(公告)日：1996-01-11
申请号：PCT/JP1995001289
申请日：1995-06-28
申请人： DAIICHI PHARMACEUTICAL CO., LTD.
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , KATO, Shozo , ITAHANA, Hidenobu , ISHIZAKI, Masahiko +di , FURUKI, Makiko , YAMAGUCHI, Masao , OHMURO, Fumio , NAGATA, Seiji , OHARA, Eiji , KITAJIMA, Toshio
IPC分类号： A61K31/275
CPC分类号： C07D213/64 , A61K31/275 , A61K31/277 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/423 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/495 , A61K31/498 , A61K31/505 , A61K31/506 , A61K31/5375 , A61K31/55 , C07C255/21 , C07D213/57 , C07D239/30 , C07D241/44 , C07D263/58 , C07D277/68 , C07D295/15 , C07D295/185 , C07D307/54 , C07D333/24
摘要： An antibacterial containing a ketonitrile derivative represented by general formula (1) or a salt thereof as the active ingredient and having an excellent antibacterial activity against Gram-positive and Gram-negative bacteria, wherein R represents hydrogen or lower alkyl; R , R , R and R represent each independently hydrogen, halogen, nitro, lower alkyl, lower alkoxy or (un)substituted phenoxy; X represents (un)substituted aromatic hydrocarbyl or (un)substituted heterocycle; Y represents (un)substituted aromatic hydrocarbyl, (un)substituted heterocycle, carbonyl substituted by (un)substituted aromatic hydrocarbyl, carbonyl substituted by (un)substituted heterocycle, or N,N-disubstituted carbamoyl.
摘要翻译：一种抗菌剂，其含有通式（1）表示的酮腈衍生物或其盐作为活性成分，对革兰氏阳性菌和革兰氏阴性菌具有优异的抗菌活性，其中R 1表示氢或低级烷基; R 2，R 3，R 4和R 5各自独立地表示氢，卤素，硝基，低级烷基，低级烷氧基或（取代的）取代的苯氧基; X表示（un）取代的芳族烃基或（un）取代的杂环; Y代表（取代的）取代的芳族烃基，（取代的）取代的杂环，由（未）取代的芳族烃基取代的羰基，被（未）取代的杂环取代的羰基或N，N-二取代的氨基甲酰基。

8. 发明申请

WO2014013261A1 PROCESS FOR CROSSED CLAISEN CONDENSATION REACTIONS PROMOTED BY LITHIUM AMIDE IN LIQUID AMMONIA 审中-公开
标题翻译：液氨酸中由钛酸铵促进的交叉分解浓缩反应的方法
公开(公告)号：WO2014013261A1
公开(公告)日：2014-01-23
申请号：PCT/GB2013/051926
申请日：2013-07-18
申请人： BAKHU PHARMA LIMITED
发明人： LEECE, Colin , PROCTOR, Lee David
IPC分类号： C07C67/343 , C07C253/30 , C01B21/092 , C07C69/63 , C07C255/21
CPC分类号： C07C67/343 , C01B21/0926 , C07C253/30 , C07C255/21 , C07C69/716
摘要： The present invention provides a use of Iithium amide in liquid ammonia as a base to produce an enolate from at least one ester starting material in a crossed Claisen condensation reaction, wherein at least one ester starting material is a β-hydroxy ester. Also provided is a method of producing lithium amide in situ for use in a crossed Claisen condensation reaction, wherein lithium is added to liquid ammonia, followed by an electron transfer agent, as well as a method of carrying out a crossed Claisen condensation reaction using an ester starting material and a β-hydroxy ester, using lithium amide in liquid ammonia produced in situ.
摘要翻译：本发明提供了在液氨中作为碱使用碘化锂作为碱，以在交叉的克莱森缩合反应中由至少一种酯原料生产烯醇化物，其中至少一种酯原料是β-羟基酯。还提供了用于交叉Claisen缩合反应中原位生产氨基化锂的方法，其中将锂加入到液氨中，随后加入电子转移剂，以及使用以下步骤进行交叉的Claisen缩合反应的方法：酯原料和β-羟基酯，使用原位生产的液氨中的氨基化锂。

9. 发明申请

WO2007014899A1 DICYANO ALKANOIC ACID AMIDES FOR COMBATING ANIMAL PESTS 审中-公开
标题翻译： DICYANO ALKANOIC ACIDES用于组合动物乳制品
公开(公告)号：WO2007014899A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064728
申请日：2006-07-27
申请人： BASF AKTIENGESELLSCHAFT , HOFMANN, Michael , BASTIAANS, Henricus, Maria, Martinus , LANGEWALD, Jürgen , OLOUMI-SADEGHI, Hassan , CULBERTSON, Deborah, L.
发明人： HOFMANN, Michael , BASTIAANS, Henricus, Maria, Martinus , LANGEWALD, Jürgen , OLOUMI-SADEGHI, Hassan , CULBERTSON, Deborah, L.
IPC分类号： A01N37/34 , C07C255/19 , C07C253/30
CPC分类号： A01N37/34 , C07C255/19 , C07C255/20 , C07C255/21 , C07C317/44
摘要： Dicyano alkanoic acid amides of formula (I), wherein R 1 is H, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, or haloalkynyl; R 2 is H, CN, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkoxy, or haloalkoxy; R 3 and R 4 are H, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, or R 3 and R 4 together can be alkylene, haloalkylene, alkenylene or haloalkenylene; X is O or S; R 5 and R 6 are H, alkyl, optionally substituted with 1 to 3 groups CN, NO 2 , OH, NR 7 R 8 , alkoxy, haloalkoxy, alkylthio, haloalkylthio, cycloalkyl, halocycloalkyl and optionally substituted phenyl; or haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, NR 7 R 8 , alkoxycarbonyl, haloalkoxycarbonyl, alkenyloxycarbonyl, haloalkenyloxycarbonyl, alkylcarbonyl, haloalkylcarbonyl, R 7 R 8 N-C(=O)-, phenylcarbonyl, benzylcarbonyl or phenyl wherein phenylcarbonyl, benzylcarbonyl and phenyl are optionally substituted; or R 5 and R 6 are a saturated, partially unsaturated or unsaturated 5- to 6-membered heterocyclic radical which may contain 1 to 4 heteroatoms selected from oxygen, nitrogen and sulfur and which radical may be bonded via a carbonyl (C(=O)) linkage, and which radical is optionally substituted; R 7 , R 8 are H, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, benzyl, phenyl, phenylcarbonyl, alkylsulfonyl, or haloalkylsulfonyl; or the enantiomers or diastereomers or salts thereof, processes for the preparation of compounds of formula (I), use of compounds of formula (I) for combating insects, acarids, or nematodes, and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites using compounds of formula (I).
摘要翻译：式（I）的二氰基链烷酸酰胺，其中R 1是H，烷基，卤代烷基，烯基，卤代烯基，炔基或卤代炔基; R 2是H，CN，烷基，卤代烷基，烯基，卤代烯基，炔基，卤代炔基，环烷基，卤代环烷基，烷氧基或卤代烷氧基。 R 3和R 4是H，烷基，卤代烷基，烯基，卤代烯基，炔基，卤代炔基，环烷基，卤代环烷基，环烯基，卤代环烯基或R 3， SO 2和R 4一起可以是亚烷基，卤代亚烷基，亚烯基或卤代亚烯基; X是O或S; R 5和R 6是H，烷基，任选被1至3个基团CN，NO 2，OH，NR 7取代烷氧基，卤代烷氧基，烷硫基，卤代烷硫基，环烷基，卤代环烷基和任意取代的苯基; 或卤代烷基，环烷基，卤代环烷基，烯基，卤代烯基，炔基，卤代炔基，烷基亚磺酰基，卤代烷基亚磺酰基，烷基磺酰基，卤代烷基磺酰基，NR 8 R 8，烷氧基羰基，卤代烷氧基羰基，烯氧基羰基，卤代链烯氧基羰基，烷基羰基，卤代烷基羰基，R 7 R 8 NC（= O） - ，苯基羰基，苄基羰基或苯基，其中苯基羰基，苄基羰基和苯基任选被取代; 或R 5和R 6是饱和的，部分不饱和的或不饱和的5至6元杂环基，其可以含有1至4个选自氧，氮和硫的杂原子并且该基团可以通过羰基（C（= O））键键合，并且该基团任选被取代; R 7，R 8是H，烷基，卤代烷基，烷基羰基，卤代烷基羰基，苄基，苯基，苯基羰基，烷基磺酰基或卤代烷基磺酰基; 或其对映体或非对映异构体或其盐，式（I）化合物的制备方法，式（I）化合物用于防治昆虫，螨虫或线虫的用途，以及用于治疗，控制，预防或保护动物的方法使用式（I）化合物对寄生虫的感染或感染。

10. 发明申请

WO2003029195A1 エポチロン誘導体の合成中間体およびそれらの製造方法审中-公开
标题翻译：用于生产这些EPOTHILONE衍生物和方法的中间体
公开(公告)号：WO2003029195A1
公开(公告)日：2003-04-10
申请号：PCT/JP2002/010089
申请日：2002-09-27
申请人：住化ファインケム株式会社
发明人：岩崎光浩 , 杉潔 , 宮本秀人 , 板谷信重
IPC分类号： C07C255/21
CPC分类号： C07D417/06 , C07B2200/07 , C07C253/30 , C07C255/21 , C07D319/06 , C07D493/04 , C07C255/12 , C07C255/20
摘要： Acetonides of a ß−keto ester compound, ß−hydroxyacid compound, and 1,3−diol derivative respectively represented by the following formulae (I), (V), and (VIII): (I) (V) (VIII) (wherein the symbols are the same as defined in the description). The acetonides are useful as intermediates for an epothilone derivative which is being developed as a drug having antitumor activity.
摘要翻译：分别由下式（I），（V）和（VIII）表示的β-酮酯化合物，β-羟基酸化合物和1,3-二醇衍生物的乙酸酯：（I）（V）（VIII）（其中符号与描述中定义的相同）。丙酮化合物可用作正在开发为具有抗肿瘤活性的药物的埃坡霉素衍生物的中间体。

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