Synthesis of protected 3′-amino nucleoside monomers
US-10035815-B2 · Jul 31, 2018 · US
Synthesis of protected 3′-amino nucleoside monomers
US10738073B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10738073-B2 |
| Application number | US-201816024221-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 29, 2018 |
| Priority date | Jul 2, 2004 |
| Publication date | Aug 11, 2020 |
| Grant date | Aug 11, 2020 |
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Abstract
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Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base.
First claim
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It is claimed: 1. A synthetic preparation of a N3′→P5′ phosphoramidate or thiophosphoramidate oligonucleotide, comprising an oligonucleotide comprising a 3′-amino-3′-deoxy nucleoside monomer having a nucleoside base which is protected with a dialkyl-, di(cycloalkyl)- or di(aralkyl)-formamidinyl group, wherein the 3′-amino nucleoside monomer is the 3′-terminal monomer. 2. The synthetic preparation of claim 1 , wherein the 3′-amino nucleoside monomer is a guanosine or an adenosine monomer. 3. The synthetic preparation of claim 1 , wherein the 3′-amino nucleoside monomer is a cytidine monomer. 4. The synthetic preparation of claim 1 , wherein the oligonucleotide comprises a deprotected 3′-amino for addition of a further monomer to the growing oligonucleotide chain. 5. The synthetic preparation of claim 1 , wherein the oligonucleotide is composed of 3′-amino-3′-deoxy nucleoside monomers independently selected from guanosine, adenosine, cytidine and thymidine, wherein all of the guanosine, adenosine and cytidine monomers have a nucleoside base which is protected with a dialkyl-, di(cycloalkyl)- or di(aralkyl)-formamidinyl group and all of the thymidine monomers have a unprotected nucleoside base. 6. A synthetic preparation of a N3′→P5′ phosphoramidate or thiophosphoramidate oligonucleotide, comprising an oligonucleotide comprising a 3′-amino-3′-deoxy nucleoside monomer having a nucleoside base which is protected with a dialkyl-, di(cycloalkyl)- or di(aralkyl)-formamidinyl group, wherein the oligonucleotide comprises a deprotected 3′-amino for addition of a further monomer to the growing oligonucleotide chain. 7. The synthetic preparation of claim 6 , wherein the 3′-amino nucleoside monomer is a guanosine or an adenosine monomer. 8. The synthetic preparation of claim 6 , wherein the 3′-amino nucleoside monomer is a cytidine monomer. 9. The synthetic preparation of claim 6 , wherein the 3′-amino nucleoside monomer is the 3′-terminal monomer. 10. The synthetic preparation of claim 6 , wherein the oligonucleotide is composed of 3′-amino-3′-deoxy nucleoside monomers independently selected from guanosine, adenosine, cytidine and thymidine, wherein all of the guanosine, adenosine and cytidine monomers have a nucleoside base which is protected with a dialkyl-, di(cycloalkyl)- or di(aralkyl)-formamidinyl group and all of the thymidine monomers have a unprotected nucleoside base.
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- What does patent US10738073B2 cover?
- Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base.
- Who is the assignee on this patent?
- Geron Corp
- What technology area does this patent fall under?
- Primary CPC classification C07H19/16. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Aug 11 2020 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 2 related publications on this page (citations in our corpus or others sharing the same primary CPC).