序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
81 Reacting Grignard compounds with carbonyl compounds and ensuing hydrolysis US955076 1997-10-21 US06054628A 2000-04-25 Manfred Stroezel; Udo Rheude; Ralf-Thomas Rahn; Gerd Kaibel
In a process for carrying out an exothermal reaction, selected from the addition reaction of organomagnesium halide compounds to carbonyl compounds and the ensuing hydrolysis of the addition product, a considerable fraction of the heat liberated during the reaction is removed by evaporation of the solvent.
82 Preparation and use of (2-butene-1,4-diyl) magnesium complexes in organic synthesis US323601 1994-10-17 US5581004A 1996-12-03 Reuben D. Rieke
The magnesium complexes of cyclic hydrocarbons and conjugated dienes, such as 1,2-dimethylenecycloalkanes and 1,3-butadienes, are readily prepared in high yields using highly reactive magnesium. Reactions of these (2-butene-1,4-diyl)magnesium reagents with electrophiles such as dibromoalkanes, alkylditosylates, alkylditriflates, bromoalkylnitriles, esters, or amides serve as a convenient method for synthesizing carbocyclic systems. Significantly, carbocycles prepared by this method contain functional groups such as the exocyclic double bond or a keto group in one of the rings which could be used for further elaboration of these molecules. Furthermore, fused bicyclic systems containing a substituted five-membered ring can be conveniently prepared at high temperatures by the reactions of (2-butene-1,4-diyl)magnesium complexes with carboxylic esters or acid halides whereas low temperatures lead to regioselective synthesis of .beta.,.gamma.-unsaturated ketones. Additionally, .gamma.-lactones, including spiro .gamma.-lactones, can be easily prepared in a one pot synthesis from the reaction of (2-butene-1,4-diyl)magnesium complexes with a ketone or aldehyde and carbon dioxide.
83 Preparation and use of (2-butene-1,4-diyl)magnesium complexes in organic synthesis US100058 1993-07-30 US5498734A 1996-03-12 Reuben D. Rieke
The magnesium complexes of cyclic hydrocarbons containing conjugated dienes, such as 1,2-dimethylenecycloalkanes, and 1,3-butadienes, are readily prepared in high yields using highly reactive magnesium. Reactions of these (2-butene-1,4 diyl)magnesium reagents with electrophiles such as dibromoalkanes, alkylditosylates, alkylditriflates, bromoalkylnitriles, esters, or amides serve as a convenient method for synthesizing carbocyclic systems. Significantly, carbocycles prepared by this method contain functional groups such as the exocyclic double bond or a keto group in one of the rings which could be used for further elaboration of these molecules. Furthermore, fused bicyclic systems containing a substituted five-membered ring can be conveniently prepared at high temperatures by the reactions of (2-butene-1,4-diyl)magnesium complexes with carboxylic esters or acid halides whereas low temperatures lead to regioselective synthesis of .beta.,.gamma.-unsaturated ketones. Additionally, .gamma.-lactones, including spiro .gamma.-lactones, can be easily prepared in a one pot synthesis from the reaction of (2-butene-1,4-diyl)magnesium complexes with a ketone or aldehyde and carbon dioxide. Also, .delta.-lactones can be easily prepared in a one pot synthesis from the reaction of (2-butene-1,4-diyl)magnesium complexes with epoxides followed by reaction with CO.sub.2. Use of .alpha.-hydroxy epoxides without the addition of CO.sub.2 leads to the synthesis of vicinal diols. Chiral epoxides lead to chiral alcohols.
84 6-aryl-6H-dibenzo[c,e][1,2]oxaphosphorine stabilizers for plastics US962187 1992-12-23 US5356967A 1994-10-18 Manfred Bohshar; Hans-Jerg Kleiner; Gerhard Pfahler
A dibenzo-[c,e] [1,2] oxaphosphorine of the formula I and process of making said compound ##STR1## wherein n=1 or 2 and in which R.sup.1 is a monovalent or divalent aromatic radical wherein a Grignard compound R.sup.1 (MgHal).sub.n is reacted with 6-chloro-6H-dibenzo[c,e][1,2] oxaphosphorine.This compound optionally with phenolic antioxidants, provides stabilization in polymers.
85 Chiral catalysts for reduction of ketones and process for their preparation US966658 1992-10-26 US5264585A 1993-11-23 Thomas J. Blacklock; Todd K. Jones; David J. Mathre; Lyndon C. Xavier
The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl- methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of diborane, borane-dimethyl sulfide or borane-tetrahydrofuran reductions of ketones to secondary alcohols.
86 Preparation and use of (2-butene-1,4-diyl)magnesium complexes in organic synthesis US763629 1991-09-23 US5231205A 1993-07-27 Reuben D. Rieke
The magnesium complexes of cyclic hydrocarbons, such as 1,2-dimethylenecycloalkanes, are readily prepared in high yields using highly reactive magnesium. Reactions of these (2-butene-1,4-diyl)magnesium reagents with electrophiles such as dibromoalkanes, alkylditosylates, or bromoalkylnitriles serve as a convenient method for synthesizing spirocyclic systems. Significantly, spirocarbocycles prepared by thisThe present invention was made with Government support under Contract No. GM35153 awarded by the National Institute of Health. The Government has certain rights in the invention.
87 Intermediates useful in the production of pesticides US428193 1989-10-27 US5068403A 1991-11-26 Michael Elliott; Norman F. Janes; Bhupinder P. S. Khambay
A process for the production of a boronic acid of formula III, ##STR1## in which an organometallic of formula IV, ##STR2## in which formula IV, M represents a metallic moiety such as --MgX, X being a halogen or an alkali metal is treated with a trialkoxy borane of formula B(OR).sub.3, R representing an alkyl group and the product is hydrolyzed.
88 Process for preparing alcohols US912220 1986-09-26 US4958033A 1990-09-18 Yukihisa Takisawa; Nobuharu Kono; Kenji Saito; Hiroshi Yamachika
A process for preparing an alcohol of the formula: ##STR1## by reacting a carbonyl compound of the formula: ##STR2## or an oxirane of the formula: ##STR3## magnesium and a propargyl halide of the formula: ##STR4## followed by hydrolysis, characterized in that the carbonyl compound (II) or the oxirane compound (III) and the propargyl halide (IV) are reacted simultaneously with magnesium in an inert solvent in the presence of zinc or a halide thereof.
89 Carboxylation of grignard reagents in the presence of liquid co2 US30627963 1963-09-03 US3360551A 1967-12-26 DAVID REGENBOGEN
90 디-유기-디알콕시실란을 제조하는 방법 KR1020147020810 2012-12-20 KR1020140117438A 2014-10-07 사이나니,자이프라카쉬브리지랠; 비말쿠마,마헨드라바이파텔; 다바드라,마헤쉬
본 발명은 디-유기-디알콕시실란, 특히 유기 치환체 중 하나 또는 둘 모두가 벌키(bulky)한 디-유기-디알콕시실란을 제조하는 방법에 관한 것이다. 이 방법은 테트라알콕시실란 화합물을 제1 그리나드(Grignard) 시약과 반응시켜 모노-유기-트리-알콕시실란 화합물을 형성시킨 뒤, 염소화제와 반응시켜 염소화된 모노-유기-디-알콕시실란을 형성시키고, 그 다음 제2 그리나드 시약과 반응시켜 디-유기-디-알콕시실란 화합물을 형성시키는 단계를 포함한다.
91 유기실레인 및 이의 유도체를 신규한 그리냐르 공정으로 제조하는 방법 KR1020047020161 2003-05-23 KR100979578B1 2010-09-01 구엔빈티
본 발명은 유기실레인의 단일 단계 제조방법에 관한 것이다. 유기실레인은 1,4-비스(다이메틸실릴)벤젠, 1,4-비스(다이메틸클로로실릴)벤젠, 및 이들의 유도체를 포함한다. 본 방법은 에터와 유기 용매의 공-용매 혼합물중에서 다이할로벤젠을 마그네슘 금속과 합하고, 이들을 하기 화학식 2의 유기규소 화합물과 반응시키는 것을 포함한다. 생성된 혼합물을 완전히 반응시킨다. 생성된 혼합물을 여과 장치를 통해 통과시킨다. 고체 마그네슘 할라이드를 함유하지 않는 액체를 분리 기법에 적용하여 목적 유기실레인을 회수한다. 화학식 2 R 2 b H c SiX d
92 비페닐 유도체의 제조 방법 KR1020087010468 2006-10-25 KR1020080066746A 2008-07-16 하야시타미오; 나카타니지로
A process for the production of biphenyl derivatives represented by the general formula (1), which is characterized by comprising reacting the chlorine atom of a benzene derivative represented by the general formula (2) with metallic magnesium to form a Grignard reagent and coupling two molecules of the Grignard reagent with each other in the presence of a catalyst and which is excellent in industrial productivity by virtue of its using inexpensive and easily available raw materials. (1) (2) (wherein A's are at least one member selected from between trifluoromethyl and fluoro; and n is an integer of 1 to 4)
93 유기실레인 및 이의 유도체를 신규한 그리냐르 공정으로 제조하는 방법 KR1020047020161 2003-05-23 KR1020050009746A 2005-01-25 구엔빈티
본 발명은 유기규소 중간체의 일 단계 제조방법에 관한 것이다. 유기규소 중간체는 1,4-비스(다이메틸실릴)벤젠, 1,4-비스(다이메틸클로로실릴)벤젠, 및 이들의 유도체와 같은 중간체를 포함한다. 본 방법은 에터 및 유기 용매의 공-용매 혼합물중에서 다이할로벤젠을 마그네슘 금속과 합하는 단계 및 이들을 하기 화학식 2의 유기규소 화합물과 반응시키는 단계를 포함한다. 생성된 혼합물을 완전하게 반응시킨다. 생성된 혼합물을 여과 장치를 통해 통과시킨다. 고체 미함유 액체의 마그네슘 할라이드에 분리 기법을 적용하여 목적 유기규소 중간체 및 이의 유도체를 회수한다. 화학식 2 R 2 b H c SiX d
94 유기 마그네슘 포스피드와 그의 제조방법, 유기 마그네슘 포스피드 착체와 그의 제조방법, 및 당해 포스피드를 사용한 유기 인계 화합물의 제조방법 KR1020197002671 2017-06-29 KR102455409B1 2022-10-14
95 디-유기-디알콕시실란을 제조하는 방법 KR1020147020810 2012-12-20 KR102010453B1 2019-08-13
96 전이 금속 촉매작용을 이용한 아릴, 헤테로아릴, 알킬 및 알켄 할로게나이드의 알릴화 및 비닐화 방법 KR1020127023324 2011-02-01 KR101536041B1 2015-07-10 고타,마티아스; 레네만,베른트빌헬름; 차플릭,발데마르막시밀리안; 마이어,마티아스; 야코비폰반겔린,악셀
본발명은하기화학식 II의해당화합물을반응시켜하기화학식 III의유기마그네슘화합물을형성한후에, 화학식 III의화합물을하기화학식 IV의화합물과반응시킴으로써하기화학식 I의유기화합물을제조하는방법이며, 화합물 III과화합물 IV의반응을, a) 화학식 II의화합물에대하여촉매량의철 화합물의존재하에, 및임의로는 b) 화학식 II의화합물에대하여촉매량또는화학량론적양의질소, 산소및/또는인을포함하는첨가제의존재하에수행하는것을특징으로하는방법에관한것이다. <화학식 I> R-R' <화학식 II> R-X 상기식에서, X는플루오린, 염소, 브로민또는아이오딘이다. <화학식 III> [M][RMgXY] <화학식 IV>
97 비페닐 유도체의 제조 방법 KR1020097003605 2007-10-12 KR101482594B1 2015-01-14 하야시타미오; 나카타니지로
저렴하고 독성이 낮은 원료를 사용함으로써 공업적으로 높은 수율로 생산성이 우수한 비페닐 유도체의 제조 방법을 제공한다. 하기 일반식(1)로 나타내어지는 비페닐 유도체의 제조 방법에 있어서, 하기 일반식(2)로 나타내어지는 벤젠 유도체의 염소 원자를 마그네슘 금속과 반응시켜 그리냐르 시약으로 전화시키고, 상기 그리냐르 시약끼리를 촉매 및 디클로로프로판의 존재 하에서 커플링 반응시키는 것을 특징으로 한다. (단, A는 알킬기, 알콕시기, 알콕시메틸기, 비닐기, 페닐기, 염소로부터 선택되는 하나 이상을 나타내고, n은 1∼4의 정수로 한다.) 비페닐 유도체의 제조 방법
98 Intermediates for the vitamin A synthesis US17676077 2022-02-18 US11851404B2 2023-12-26 Raphael Beumer; Werner Bonrath; Marc-André Mueller; Bettina Wüestenberg
Processes for synthesizing new compounds that may usefully be employed in organic synthesis, especially in the synthesis of vitamin A or β-carotene and derivatives thereof, e.g. canthaxanthin, astaxanthin or zeaxanthin are disclosed. The new compounds are especially useful as intermediates (building blocks) in the synthesis of vitamin A or β-carotene, preferably vitamin A.
99 Process for preparation of palbociclib US16314972 2017-07-03 US10807978B2 2020-10-20 Andiappan Murugan; Vipinkumar Shriram Kabra; Chinna Saida Reddy Gade; Rama Rao Gondu; Shravankumar Chandrashekar; Krishnamoorthy Pasupathy; Anandan Kalaiselvan
The present application relates to a process for the preparation of crystalline form A of palbociclib having specific surface area more than 2 m2/g comprising one-pot process for the preparation of compound of formula (IV). The present application further relates to the preparation of acid-addition salts of palbociclib and their use for the synthesis of crystalline form A of palbociclib having specific surface area more than 2 m2/g.
100 PROCESS FOR PREPARATION OF PALBOCICLIB US16314972 2017-07-03 US20190241561A1 2019-08-08 Andiappan MURUGAN; Vipinkumar Shriram KABRA; Chinna Saida Reddy GADE; Rama Rao GONDU; Shravankumar CHANDRASHEKAR; Krishnamoorthy PASUPATHY; Anandan KALAISELVAN
The present application relates to a process for the preparation of crystalline form A of palbociclib having specific surface area more than 2 m2/g comprising one-pot process for the preparation of compound of formula (IV). The present application further relates to the preparation of acid-addition salts of palbociclib and their use for the synthesis of crystalline form A of palbociclib having specific surface area more than 2 m2/g.
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