Hydroxy- or thiol-substituted amino acids are t-butylated by reacting them with isobutylene in the presence of a catalyst comprising boron trifluoride and anhydrous phosphoric acid.
Edward L. Smithwick - Indianapolis IN Robert C. A. Frederickson - Indianapolis IN Robert T. Shuman - Greenwood IN
International Classification:
C07C10352
US Classification:
2601125E
Abstract:
Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D, when applicable, define the chirality; R. sub. 1 and R. sub. 2 independently are hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 3 is C. sub. 1 -C. sub. 4 primary or secondary alkyl or --CH. sub. 2 CH. sub. 2 --S--CH. sub. 3 ; R. sub. 4 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 5 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; Y is hydrogen or acetyl; and Z is ##STR2## --CH. sub. 2 OH, or --CN; subject to the limitation that no more than one of R. sub. 4 and R. sub. 5 is C. sub. 1 -C. sub. 3 primary alkyl; are useful analgesic agents.
Crosslinked Polystyrene And Substituted Polystyrene Compositions
A composition which is either polystyrene or a substituted polystyrene crosslinked with divinylbenzene and swollen by N-methyl-2-pyrrolidone, which composition is useful in purifying blocked synthetic peptides by means of gel exclusion chromatography and in solid-phase peptide synthesis.
Edward L. Smithwick - Indianapolis IN Robert C. A. Frederickson - Indianapolis IN Robert T. Shuman - Greenwood IN
Assignee:
Eli Lilly and Company - Indianapolis IN
International Classification:
C07C10352
US Classification:
2601125R
Abstract:
Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D, when applicable, define the chirality; R. sub. 1 is hydrogen, C. sub. 1 -C. sub. 3 primary alkyl, or allyl; R. sub. 2 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl, subject to the limitation that when R. sub. 1 is allyl, R. sub. 2 is hydrogen; R. sub. 3 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 4 is C. sub. 1 -C. sub. 4 primary or secondary alkyl; R. sub. 5 is hydrogen or C. sub. 1 -C. sub. 4 primary or secondary alkyl; R. sub. 6 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 7 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; Y is hydrogen or acetyl; Z is hydrogen of ##STR2## in which R. sub. 8 is C. sub. 1 -C. sub. 3 alkyl or hydrogen; and W is isopropyl, --VR. sub.
Edward L. Smithwick - Indianapolis IN Robert C. A. Frederickson - Indianapolis IN Robert T. Shuman - Greenwood IN
Assignee:
Eli Lilly and Company - Indianapolis IN
International Classification:
C07C10352
US Classification:
2601125E
Abstract:
Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in which: L and D, when applicable, define the chirality; R. sub. 1 is hydrogen, C. sub. 1 -C. sub. 3 primary alkyl, or allyl; R. sub. 2 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl, subject to the limitation that when R. sub. 1 is allyl, R. sub. 2 is hydrogen; R. sub. 3 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 4 is C. sub. 1 -C. sub. 4 primary or secondary alkyl; R. sub. 5 is hydrogen or C. sub. 1 -C. sub. 4 primary or secondary alkyl; R. sub. 6 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 7 is hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; Y is hydrogen or acetyl; Z is hydrogen or ##STR2## in which R. sub. 8 is C. sub. 1 14 C. sub. 3 alkyl or hydrogen; and W is isopropyl, --VR. sub.
Edward L. Smithwick - Indianapolis IN Robert C. A. Frederickson - Indianapolis IN Robert T. Shuman - Greenwood IN
Assignee:
Eli Lilly and Company - Indianapolis IN
International Classification:
C07C10352 A61K 3700
US Classification:
2601125R
Abstract:
Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D define the chirality; R. sub. 1 and R. sub. 2 independently are hydrogen or C. sub. 1 -C. sub. 3 primary alkyl; R. sub. 3 is C. sub. 1 -C. sub. 4 primary or secondary alkyl, C. sub. 1 -C. sub. 2 hydroxyalkyl, or --CH. sub. 2 CH. sub. 2 --U--CH. sub. 3, in which U is O or S; R. sub. 4 is C. sub. 1 -C. sub. 3 primary alkyl; Y is hydrogen or acetyl; Z is --CH. sub. 2 OH or ##STR2## in which R. sub. 5 is C. sub. 1 -C. sub. 3 alkyl or hydrogen; and W is isopropyl, --VR. sub. 6, or --CH. sub. 2 --X--CH. sub. 3, in which V is O or S, R. sub. 6 is C. sub. 1 -C. sub. 4 alkyl or aralkyl, and X is O, S, or CH. sub. 2 --; are useful analgesic agents.
Jesse L. Bobbitt - Indianapolis IN Edward L. Smithwick - Indianapolis IN
Assignee:
Eli Lilly and Company - Indianapolis IN
International Classification:
C07C10352
US Classification:
2601125R
Abstract:
The proteinase plasmin is assayed either colorimetrically or fluorometrically with a tripeptidyl-4-methoxy-2-naphthylamide substrate having the following general formula: ##STR1## The substrate is useful for either routine clinical assays or kinetic studies.