# US 4,394,519 A · Amino acid blocking agents

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- Number: US 4,394,519 A
- Document ID: US4394519A
- Status: Granted
- Kind: A
- Application number: 06/342,296
- Filed: 1982-01-19
- Granted: 1983-07-19
- Earliest claimed: 1982-01-19
- Assignees: Research Corporation
- Inventors: Louis A. Carpino; Beri Cohen
- Web page: https://patentgrep.com/patent/US4394519A

## CPC

- C07K 5/0827: {containing heteroatoms different from O, S, or N}
- C07C 29/14: of a —CHO group
- C07C 45/00: Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07K 1/063: {for alpha-amino functions}
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Process for the preparation of peptides including higher polypeptides utilizing indenylmethoxycarbonyl blocking groups and products produced thereby.

## Claims

### Claim 1

A protected amino acid of the formula: ##STR20## wherein R is an amino acid residue; R.sub.3 and R.sub.4 are each hydrogen, alkyl, aryl or aralkyl; R.sub.5 is up to three hydrogen atoms, alkyl, aryl, alkaryl aralkyl, halogen or nitro; and R.sub.6 is up to four hydrogen atoms, fused phenyl, alkyl, aryl, alkaryl, aralkyl, halogen or nitro; the alkyl, aryl, alkaryl or aralkyl group containing up to nine carbon atoms.

### Claim 2 (depends on 1)

A protected amino acid of claim 1 wherein R.sub.3, R.sub.4 and R.sub.6 are hydrogen and R.sub.5 is a 2-halogen.

### Claim 3 (depends on 2)

A protected amino acid of claim 2 wherein R.sub.5 is 2-chloro.

### Claim 4 (depends on 1)

A protected amino acid of claim 1 wherein R.sub.3, R.sub.4 and R.sub.6 are hydrogen and R.sub.5 is 2-phenyl.

### Claim 5

N-(2-chloro-1-indenylmethoxycarbonyl)phenylalanine.

### Claim 6

N-(2-chloro-1-indenylmethoxycarbonyl)glycine.

### Claim 7

N-(1-indenylmethoxycarbonyl)glycine.

### Claim 8

N-(1-benz(f) indenylmethoxycarbonyl)glycine.

### Claim 9

N-(2-phenyl-1-indenylmethoxycarbonyl)glycine.