# US 2016/0102118 A1 · Solid phase peptides synthesis processes and associated systems

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- Number: US 2016/0102118 A1
- Document ID: US20160102118A1
- Status: Published application
- Kind: A1
- Application number: 14/853,683
- Filed: 2015-09-14
- Published: 2016-04-14
- Earliest claimed: 2013-03-15
- Assignees: Massachusetts Institute of Technology
- Applicants: Massachusetts Institute of Technology
- Inventors: Mark David Simon; Bradley L. Pentelute; Andrea Adamo; Patrick Louis Heider; Klavs F. Jensen
- Web page: https://patentgrep.com/patent/US20160102118A1

## CPC

- C07K 1/045: {using devices to improve synthesis, e.g. reactors, special vessels}
- B01J 8/00: Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes
- B01J 19/00: Chemical, physical or physico-chemical processes in general; Their relevant apparatus
- B01J 19/0053: {Details of the reactor}
- C07K 1/04: on carriers {(C07K1/003, C07K1/006 take precedence)}
- C07K 1/042: {characterised by the nature of the carrier}
- C07K 1/061: {using protecting groups}
- C07K 1/08: using activating agents {(C07K1/003, C07K1/006 take precedence)}
- 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)
- B01J: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS

## Abstract

Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.

## Claims

### Claim at position 1

1-17. (canceled)

### Claim 18

A process for adding amino acid residues to peptides, comprising:
flowing a first stream comprising amino acids;
flowing a second stream comprising an amino acid activating agent;
merging the first and second streams to form a mixed fluid comprising activated amino acids; and
within about 30 seconds after merging the first and second streams to form the mixed fluid, exposing the mixed fluid to a plurality of peptides immobilized on a solid support.

### Claim 19 (depends on 18)

The process of claim 18, wherein the amino acid activating agent comprises an alkaline liquid, a carbodiimide, and/or a uronium activating agent.

### Claim at position 4

20-23. (canceled)

### Claim 24 (depends on 18)

The process of claim 18, wherein the solid support comprises polystyrene and/or polyethylene glycol.

### Claim 25 (depends on 18)

The process of claim 18, wherein the solid support comprises a resin.

### Claim 26 (depends on 25)

The process of claim 25, wherein the solid support comprises a microporous polystyrene resin.

### Claim 27 (depends on 18)

The process of claim 18, wherein the solid support is contained within a packed column and/or a fluidized bed.

### Claim 28 (depends on 18)

The process of claim 18, wherein an amino acid residue is added to at least about 99% of the immobilized peptides after exposing the mixed fluid to the immobilized peptides.

### Claim 29 (depends on 18)

The process of claim 18, wherein multiple copies of the amino acid residue are bonded to fewer than about 1% of the immobilized peptides after exposing the mixed fluid to the immobilized peptides.

### Claim 30 (depends on 28)

The process of claim 28, wherein adding an amino acid residue to the immobilized peptides comprises adding a single amino acid residue to the immobilized peptides.

### Claim 31 (depends on 28)

The process of claim 28, wherein adding an amino acid residue to the immobilized peptides comprises adding a peptide comprising two or more amino acid residues to the immobilized peptides.

### Claim at position 13

32-71. (canceled)

### Claim 72 (depends on 18)

The process of claim 18, comprising exposing the mixed fluid to the plurality of peptides immobilized on the solid support within about 15 seconds after merging the first and second streams to form the mixed fluid.

### Claim 73 (depends on 18)

The process of claim 18, comprising exposing the mixed fluid to the plurality of peptides immobilized on the solid support within about 10 seconds after merging the first and second streams to form the mixed fluid.

### Claim 74 (depends on 18)

The process of claim 18, comprising exposing the mixed fluid to the plurality of peptides immobilized on the solid support within about 5 seconds after merging the first and second streams to form the mixed fluid.

### Claim 75 (depends on 18)

The process of claim 18, wherein the amino acids comprise protection groups.

### Claim 76 (depends on 75)

The process of claim 75, wherein amine groups of the amino acids are protected.

### Claim 77 (depends on 75)

The process of claim 75, wherein the protection groups comprise fluorenylmethyloxycarbonyl protection groups.

### Claim 78 (depends on 75)

The process of claim 75, wherein the protection groups comprise tertbutyloxycarbonyl protection groups.

### Claim 79 (depends on 75)

The process of claim 75, wherein the protection groups comprise allyloxycarbonyl protection groups.

### Claim 80 (depends on 75)

The process of claim 75, wherein the protection groups comprise carboxybenzyl protection groups.