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7022841 |
Process for making carbapenem compounds
The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by...
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5547667 |
Linker for bioactive agents
Conjugates of general formula 1: [A--O--W--Z] a --T 1 wherein the moiety A--O-- is the residue of drug of formula A--O--H in which --O--H is a primary or...
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4619787 |
Beta lactams
The novel compounds of the formula ##STR1## wherein R 1 is hydrogen, a residue readily removable by reduction, lower 1-hydroxyalkyl or lower alkanoyl and R 2 is hydrogen, or each of R 1 and R...
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4529545 |
Isolation of chemically unstable antibiotics from fermentation solutions
A method for isolating a chemically unstable carbapenem antibiotic from a fermentation solution by adsorbing the antibiotic on an ion exchanger resin at the maximum of product formation, thus...
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4499278 |
Trans-3-carboxymethylene-4-carboxy-5-methyl-delta2-isoxazoline as intermediate
Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R 5 and R 6 are removable protecting groups.
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4460507 |
Process for the preparation of thienamycin
Disclosed is a process for the total synthesis of thienamycin from descysteaminylthienamycin 1 ##STR1## via thienamycin sulfoxide 4: ##STR2## R 3 , R°, R' are blocking groups.
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4438036 |
β-Lactam antibiotics their preparation and their use
The present invention provides a process for inversion of the absolute stereochemistry at the α-carbon atom of a C-6 substituent of a bicyclic carbapenem antibiotic via a phosphorus -...
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4414155 |
Synthesis of thienamycin via esters of (3SR, 4RS)-3-[(SR)-1-hydroxyethyl]-β,2-dioxo-4-azetidinebutanoic acid
Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R 3 is a readily removable carboxyl protecting group.
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4400323 |
3-[1-Hydroxyethyl]-4-carboxymethyl-azetidin-2-one
In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## there is disclosed a process for preparing III via ##STR2## wherein R is a protecting group.
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4386029 |
Process for the preparation of antibiotics
The present invention provides a process for the preparation of a compound of the formula (O): ##STR1## wherein R° is SCH 2 CH 2 NH 2 which process comprises the reaction of a cleavable ester...
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4383946 |
Process for the preparation of 1-carbapenems and intermediates via silyl-substituted dithioacetals
Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via central intermediates II and III: ##STR1## wherein R is hydrogen, a pharmaceutically...
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4356120 |
3-(1-Hydroxyethyl)-4-(but-2-ene)-azetidin-2-one and derivatives
Disclosed is a process for the total synthesis of thienamycin from substituted 4-allylazetidinone (IIIa) via intermediate III: ##STR1## wherein: R=H, blocking group or a salt cation; and R° is...
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4349687 |
Intermediate for synthesis of thienamycin via (3SR, 4RS)-3-[1 (SR)-hydroxyethyl]-2-oxo-4-azetidineacetic acid
Disclosed is a process for the stereocontrolled total synthesis of thienamycin via intermediates II and IIa: ##STR1## wherein R is a readily removable carboxyl protecting group.
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4348320 |
Substituted azetidiones
Disclosed are substituted azetidinones (1) which are useful in the preparation of 1-carba-2-penem-3-carboxylic acids (I): ##STR1## wherein R is hydrogen or a blocking group and R 1 , R 2 and R 3 ...
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4347368 |
3 -Substituted-6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxyl ic acid
Disclosed are 3- and 6-substituted 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein R 6 , R 7 and R 8 are, inter alia, independently selected from the...
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4347367 |
3-Substituted-6-(1'-hydroxyethyl)-7-oxo-1-azabicyc lo[3.2.0]-hept-2-ene-2-carboxylic acid
Disclosed are 3-substituted-6-(1'-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]h
ept-2-ene-2-ca rboxylic acids having the structure: ##STR1## wherein R 8 is, inter alia, selected from the group...
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4344885 |
Intermediate for the preparation of thienamycin
Disclosed is a process for the stereocontrolled total synthesis of thienamycin from acetone dicarboxylate via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group.
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4341706 |
Process for the preparation of carbapenem antibiotics
Disclosed is a process for the synthesis of carbapenem antibiotics I and their pharmaceutically acceptable salts and esters from 1: ##STR1## wherein: R 7 , R 6 , R 1 , R 2 and R 8 are selected...
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4341791 |
6-, 2- and 1,1-Disubstituted-1-carbadethiapen-2-em-3-carboxylic acid S-oxides
Disclosed are S-oxides of 6-, 2- and 1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R 1 , R 2 , R 6 , R 7 and R 8 are, inter...
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4312871 |
6-, 1- And 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids
Disclosed are 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: R 1 , R 2 , R 6 , R 7 and R 8 are, inter alia, independently selected from...
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4309346 |
Process for the preparation of 1-carbapenems and intermediates via trithioorthoacetates
Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via intermediates II and III: ##STR1## wherein R is hydrogen, a pharmaceutically acceptable ester...
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4282322 |
Process for enzymatic deacylation of antibiotics
This invention relates to two new antibiotics, desacetyl 890A 1 and desacetyl 890A 3 , active against both gram-positive and gram-negative bacteria, which are produced by treating 890A 1 and 890A...
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4269772 |
Synthesis of thienamycin via trans-3-carboxymethylene-4-carboxy-5-methyl-Δ.sup.2 -isoxazoline
Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R 5 and R 6 are removable protecting groups.
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4234596 |
3-(2-Aminoethyl thio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
Isomeric forms of 3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3
.2.0]hept-2-en e-2-carboxylic acid (I) ##STR1## are disclosed; also disclosed is a process for their total synthesis;...
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4212807 |
Process for deacylating N-acyl-6-substituted-2-[2-aminoethylthio]-1-carbadethiapen-2-em-3-carbox ylic acids
Disclosed is a process for chemically cleaving the acyl group from N-acyl-6-substituted-2-[2-aminoethylthio]-1-carbadethiapen-2
-em-3-carboxyl ic acids which proceeds via an imino chloride...
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4211707 |
Process for hydrolytically cleaving O-sulfo thienamycins
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...
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4203902 |
Process for preparing 6- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids
A process is disclosed for preparing antibiotic 6- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids and their pharmaceutically acceptable salts and esters (I) ##STR1## wherein: R 1 and R...
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4198338 |
Process for purifying thienamycin
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...
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4168268 |
Process for isolating thienamycin
Fermentation broths or impure solutions containing thienamycin, a substance having antibiotic activity against gram-negative and gram-positive microorganisms, are isolated using liquid ion exchange...
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4000161 |
Process for purifying thienamycin
Fermentation broths or impure solutions containing thienamycin, a substance having antibiotic activity against gram-negative and gram-positive microorganisms, are purified using ion exchange...
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