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序号	专利名	申请号	申请日	公开（公告）号	公开（公告）日	发明人
41	Alkylation process for preparing azetidinone compound and starting compound therefor	US262892	1994-06-21	US5550229A	1996-08-27	Tameo Iwasaki; Kazuhiko Kondo; Hiroshi Ohmizu
Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.
42	Optically active pyrrolidine derivative	US915808	1992-09-15	US5342963A	1994-08-30	Kuniya Sakurai; Kunisuke Izawa; Hiroyuki Izawa; Takashi Ineyama; Tomihisa Ohta; Shigeo Nozoe
Optically active pyrrolidine derivative represented by the following formula (XI): ##STR1## wherein R.sup.1 represents a benzyl group R.sup.2 represents an alkyl group having 1 to 6 carbon atoms, R.sup.3 represents an alkyl group having 1 to 6 carbon atoms, a benzyl group or an allyl group, R.sup.4 is selected from the group consisting of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms which may be substituted with a protected hydroxyl group, a vinyl group, a phenyl group which may be substituted, a benzyl group which may be substituted, and a heterocyclic ring having 1 to 4 nitrogen or/and oxygen atoms, and R.sup.5 represents a hydrogen atom or a methyl group.This compound can be an intermediate for synthesis of carbapenem antibiotic compounds.
43	Process for producing 2-carbon-substituted carbapenem derivatives	US989150	1992-12-11	US5258509A	1993-11-02	Susumu Nakagawa; Yoshiaki Kato; Hiroshi Fukatsu
A process for producing a 2-(unsubstituted or carbon-substituted)-1-carbapen-2-em-3-carboxylic acid derivative, which comprises reacting a 2-trifluoromethanesulfonyloxy-1-carbapen-2-em-3-carboxylic acid derivative or the 1-carbapen-2-em-3-carboxylic acid derivative derived from a 2-oxo-1-carbapenam-3-carboxylic acid derivative and trifluoromethanesulfonic anhydride, and a stannane derivative in an inert solvent in the presence of a palladium compound and a salt.
44	Process for producing halomethylcarbapenems	US594942	1990-10-10	US5064954A	1991-11-12	Shoichiro Uyeo; Mitsuru Imuta; Hisao Ona; Hikaru Itani
A functionallized intermediate for antibacterial carbapenems, 2-halomethylcarbapenem (III) is effectively synthesized by treating 2-hydroxymethylcarbapenem (I) with a phosphorylating reagent to give 2-phosphoryloxymethylcarbapenem (II) and then treating this product with a halogenating reagent. Some carbapenems derived from the intermediate are also disclosed. ##STR1## wherein, R.sup.1 is hydrogen or substituted or unsubstituted alkyl;R.sup.2 is hydrogen or substituted or unsubstituted alkyl;R.sup.3, R.sup.4 is halogen or substituted or unsubstituted alkoxy or aryloxy;R.sup.5 is hydrogen or carboxy protecting group; andHal is halogen.
45	Process for preparing 3-substituted-6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carbox ylic acid	US759721	1985-07-29	US4745188A	1988-05-17	Burton G. Christensen; Ronald W. Ratcliffe
Disclosed is a process for preparing 3- and 6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids: ##STR1## wherein: X is a leaving group such as chloro, bromo, tosyl, mesyl or the like; and R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds (I), as well as their pharmaceutically acceptable salt, ester and amide derivatives, are useful as antibiotics.
46	Process for producing an antibiotic	US296306	1981-08-26	US4415497A	1983-11-15	Masahito Nakayama; Shigeru Kimura; Toshimi Mizoguchi; Sohei Tanabe; Toshihito Mori
An antibiotic KA-6643-A or a salt thereof having the formula: ##STR1## is produced by a process comprising the step of hydrolyzing an antibiotic KA-6643-B of the formula: ##STR2##
47	Thienamycin derivatives	US195993	1980-10-10	US4341705A	1982-07-27	David H. Shih
Disclosed is a process for the total synthesis of thienamycin from descysteaminylthinamycin 1 ##STR1## via thienamycin sulfoxide 4: ##STR2## R.sup.3, R.degree., R' are blocking groups.
48	Process for hydrolytically cleaving O-sulfo thienamycins	US932739	1978-08-10	US4211707A	1980-07-08	Ronald W. Ratcliffe
Disclosed is a process for the hydrolytically cleaving O-sulfo thienamycins: ##STR1## wherein R is H or acetyl and M is H, an alkali or alkaline earth metal cation or an organo cationic species such as pyridinium; and wherein the dotted line indicates saturated and unsaturated species.
49	Process for purifying thienamycin	US885836	1978-03-13	US4198338A	1980-04-15	Laszlo R. Treiber; Vincent P. Gullo
Fermentation broths or impure solutions containing thienamycin, a substance having antibiotic activity against gram-negative and gram-positive microorganisms, are purified using a sequence of ion exchange resins, starting with an anion exchange resin of the polystyrene-trimethylammonium type in the HCO.sub.3 -cycle, and ending with absorption on and elution from a polymeric cross-linked polystyrene-type resin adsorbent. Variations in the intermediate steps, e.g. different resins and eluates are possible and are illustrated within.
50	.DELTA..sup.3 -Thienamycin	US847292	1977-10-31	US4146633A	1979-03-27	Burton G. Christensen; Ronald W. Ratcliffe; David H. Shih
The antibiotic .DELTA..sup.3 -thienamycin is disclosed: ##STR1## It is prepared by double bond isomerization of thienamycin. Also disclosed are pharmaceutical compositions comprising .DELTA..sup.3 -thienamycin, and methods of treatment comprising administering .DELTA..sup.3 -thienamycin when an antibiotic effect is indicated.
51	Intermediates for pyrrolidylthiocarbapenem derivative	US574863	1995-12-19	US5703243A	1997-12-30	Yasuhiro Nishitani; Tadashi Irie; Yutaka Nishino
A pyrrolidylthiocarbapenem derivative represented by Formula I is provided: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sufamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group.
52	Metal catalyzed displacement process	US459542	1995-06-02	US5681951A	1997-10-28	Koichi Hirai; Yuji Iwano; Takahide Nishi; Akira Yoshida; Kozo Oda; Hiroo Koyama
A process for preparing a compound of formula (I'): ##STR1## comprising reacting a compound of formula (II'): ##STR2## with a compound of formula (III'): A'SH (III') wherein the reaction of the compound of formula (II') and the compound of formula (III') are carried out in the presence of a salt of a metal of Group II or III of the Periodic Table of Elements, wherein A' is an alkyl, aryl, aralkyl or heterocyclic, R.sup.1' is hydrogen or a carboxy protecting group, R.sup.2' and R.sup.3' can be hydrogen or alkyl, X' can be sulfur, k' is 1 or 2 and R.sup.4' is alkyl, alkenyl, aryl, aralkyl, cycloalkyl or heterocyclic.
53	Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor	US409410	1995-03-24	US5495012A	1996-02-27	Tameo Iwasaki; Kazuhiko Kondo; Tadashi Nakatani; Ryuzo Yoshioka
A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula [I]: ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group and R.sup.2 is a hydrogen atom or a protecting group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.
54	Adhesive composition	US204929	1994-03-01	US5480720A	1996-01-02	Eric K. Eisenhart; Louis C. Graziano; Jose P. Lalas
An adhesive composition includes from about 30 weight percent to about 70 weight percent solids dispersed in an aqueous medium. The solids include from about 60 weight percent to about 97.9 weight percent of a polymer having a glass transition temperature of about -40.degree. C. to about 10.degree. C. and including first repeating units derived from an alkyl (meth)acrylate monomer, a vinyl ester monomer, a styrenic monomer or a mixture thereof and second repeating units derived from a hydroxyalkyl (meth)acrylate monomer, a monoethylenically unsaturated nitrogenous monomer or a mixture thereof; from about 2 weight percent to about 30 weight percent of a polyfunctional epoxy resin including two or more epoxide groups per molecule; from about 0.1 weight percent to about 10 weight percent of a polyfunctional curing agent including two or more amino groups or amido groups per molecule; and from about 0.01 weight percent to about 30 weight percent of a metal salt. A method for making a laminate includes applying a layer of the aqueous adhesive composition to a first substrate layer and covering the layer of adhesive composition with a second substrate layer to form the laminated article. A laminate includes two substrate layers bonded together by an interposed layer of the solids of the adhesive composition.
55	Preparation of 2-aryl carbapenems via a boronic acid coupling reaction	US226788	1994-04-12	US5442057A	1995-08-15	Ann Decamp; Ulf H. Dolling; Yulan Li; Dale L. Rieger; Nobuyoshi Yasuda; Lyndon C. Xavier
The present invention is directed to a process of making 2-Aryl Carbapenems of Formula 1 from a compound of formula 2. ##STR1##
56	Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor	US166866	1993-12-15	US5424446A	1995-06-13	Tameo Iwasaki; Kazuhiko Kondo; Tadashi Nakatani; Ryuzo Yoshioka
A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula: ##STR1## wherein a group of the formula: --SR.sup.1 is a protected or unprotected mercapto group, and the group of the formula: .dbd.NR.sup.2 is a protected or unprotected imino group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(2,3,4-trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.
57	Pyrrolidylthiocarbapenem derivative	US929961	1992-08-14	US5317016A	1994-05-31	Yasuhiro Nishitani; Tadashi Irie
A pyrrolidylthiocarbapenem derivative represented by Formula I is provided: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sufamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group.
58	Process for making antimicrobial quinolonyl lactams	US59529	1993-05-07	US5281703A	1994-01-25	Ronald E. White; Thomas P. Demuth, Jr.
The present invention provides methods of making compounds of the structure[Q-L.sup.1 ]-L-[L.sup.2 -B[wherein(I) Q is a quinolone moiety;(II) B is a beta-lactam moiety;(III) L, L.sup.1, and L.sup.2 together comprise a carbamate-containing linking moietycomprising the steps of:(1) Reacting a lactam compound of the formula B-L.sup.4 -H with phosgene to form an intermediate compound of the formula B--L.sup.4 --C(=O)--Cl, where L.sup.4 is oxygen; and(2) Coupling said intermediate compound with a quinolone compound of the formula Q-L.sup.3 -R.sup.44 ; wherein L.sup.3 is nitrogen; R.sup.44 is hydrogen, Si(R.sup.45).sub.3, or Sn(R.sup.45).sub.3 ; and R.sup.45 is lower alkyl.Preferably, the process additionally comprises steps prior to the reacting and coupling steps where esters of the lactam and quinolone compounds are made. Also preferably, the coupling step comprises adding a solution containing the quinolone compound to a solution containing the intermediate compound. The process steps are also preferably performed at a temperature of from about -80.degree. C. to about 0.degree. C. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem.
59	Method for removing the protecting group for hydroxy group	US52680	1993-04-27	US5260438A	1993-11-09	Hiroshi Horikawa; Kazuhiko Kondo; Tameo Iwasaki
A method for removing tri-substituted silyl group from .beta.-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.
60	Process for the preparation of bis(aryl)-phosphorohalidates	US966786	1992-10-27	US5245069A	1993-09-14	James W. McManus
This invention relates to a novel process for preparing bis(aryl)phosphorohalidates which are useful in the synthesis of various enol phosphates. The process of this invention provides a means of producing a high-yield, high-purity product without the need for costly crystallization or impractical, high temperature distillations.

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