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Saxagliptin Hydrate
Tier B — Position earlySaxagliptin Hydrate
Bristol Myers Squibb
Originator
2009
First approval
-
Expiry (public)
$1.25B ▲
Peak sales
Small molecule
Type
Targets：DPP4
Brand：Onglyza
Indications (approved)：Type 2 diabetes
Regional status
US
Withdrawn
EU
Approved
2009-09-30
China
Approved
2011-05-05
Japan
Approved
2013-03-25
Synthetic routes & intermediates4 routes
Originator routes × 1Optimised (non-patent) × 3Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OriginatorRoute 1Steps 11 · Total yield /
SAXA-00198-79-3SAXA-0027149-65-7SAXA-003144978-12-1SAXA-004178172-26-4SAXA-00590104-21-5SAXA-006709031-38-9SAXA-007361440-67-7SAXA-008709031-45-8SAXA-009361442-01-5SAXA-0101194836-75-3SAXA-011709031-43-6SAXA-012361442-00-4SAXA-013768-90-1SAXA-01469097-20-7SAXA-01530074-09-0SAXA-016128665-98-5SAXA-017709031-32-3SAXA-018709031-33-4SAXA-019709031-28-7SAXA-020709031-29-8SAXA-021598-99-2SAXA-022199783-35-2SAXA-023709031-34-5SAXA-024709031-35-6SAXA-025709031-36-7SAXA-0264942-47-6SAXA-02759768-70-6SAXA-028317375-33-0SAXA-029709031-30-1SAXA-030—API · Saxagliptin Hydrate
| Code | CAS No. | Intermediate |
|---|---|---|
| SAXA-001 | 98-79-3Available | (S)-5-oxopyrrolidine-2-carboxylic acid |
| SAXA-002 | 7149-65-7 | (S)-ethyl 5-oxopyrrolidine-2-carboxylate |
| SAXA-003 | 144978-12-1 | 1-(tert-butyl) 2-ethyl (S)-5-oxopyrrolidine-1,2-dicarboxylate |
| SAXA-004 | 178172-26-4Available | 1-(tert-butyl) 2-ethyl (S)-2,3-dihydro-1H-pyrrole-1,2-dicarboxylate |
| SAXA-005 | 90104-21-5 | (S)-1-(tert-butoxycarbonyl)-2,3-dihydro-1H-pyrrole-2-carboxylic acid |
| SAXA-006 | 709031-38-9 | tert-butyl (S)-2-carbamoyl-2,3-dihydro-1H-pyrrole-1-carboxylate |
| SAXA-007 | 361440-67-7Available | tert-butyl (1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexane-2-carboxylate |
| SAXA-008 | 709031-45-8Available | (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide methanesulfonate |
| SAXA-009 | 361442-01-5 | tert-butyl ((S)-2-((1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexan-2-yl)-1-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoethyl)carbamate |
| SAXA-010 | 1194836-75-3 | (1R,3r,5R,7S)-3-((S)-1-((tert-butoxycarbonyl)amino)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)adamantan-1-yl 2,2,2-trifluoroacetate |
| SAXA-011 | 709031-43-6 | tert-butyl ((S)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-1-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoethyl)carbamate |
| SAXA-012 | 361442-00-4Available | (S)-2-((tert-butoxycarbonyl)amino)-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-013 | 768-90-1 | (3s,5s,7s)-1-bromoadamantane |
| SAXA-014 | 69097-20-7 | 2,2,7,7-tetramethyl-4-((trimethylsilyl)oxy)-3,6-dioxa-2,7-disilaoct-4-ene |
| SAXA-015 | 30074-09-0 | 2-((3r,5r,7r)-adamantan-1-yl)-2-hydroxyacetic acid |
| SAXA-016 | 128665-98-5 | methyl 2-((3r,5r,7r)-adamantan-1-yl)-2-hydroxyacetate |
| SAXA-017 | 709031-32-3 | methyl 2-((3r,5r,7r)-adamantan-1-yl)-2-oxoacetate |
| SAXA-018 | 709031-33-4 | methyl 2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoacetate |
| SAXA-019 | 709031-28-7 | 2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoacetic acid |
| SAXA-020 | 709031-29-8 | (S)-2-amino-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-021 | 598-99-2 | methyl 2,2,2-trichloroacetate |
| SAXA-022 | 199783-35-2 | ((2,2-dichloro-1-methoxyvinyl)oxy)trimethylsilane |
| SAXA-023 | 709031-34-5 | methyl 2-((3r,5r,7r)-adamantan-1-yl)-2,2-dichloroacetate |
| SAXA-024 | 709031-35-6 | methyl 2,2-dichloro-2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)acetate |
| SAXA-025 | 709031-36-7 | 2,2-dichloro-2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-026 | 4942-47-6 | 2-((3r,5r,7r)-adamantan-1-yl)acetic acid |
| SAXA-027 | 59768-70-6 | 2-((3r,5r,7r)-adamantan-1-yl)-2-bromoacetic acid |
| SAXA-028 | 317375-33-0 | 2-bromo-2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-029 | 709031-30-1 | 2-amino-2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-030 | - | 2-((tert-butoxycarbonyl)amino)-2-((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
OptimisedRoute 2Steps 11 · Total yield /
SAXA-009361442-01-5SAXA-031828-51-3SAXA-032711-01-3SAXA-033770-71-8SAXA-0342094-74-8SAXA-035—SAXA-036361441-95-4SAXA-037361441-96-5SAXA-03895853-35-3SAXA-039361441-97-6SAXA-040361442-00-4SAXA-041361440-69-9API · Saxagliptin Hydrate
| Code | CAS No. | Intermediate |
|---|---|---|
| SAXA-009 | 361442-01-5 | tert-butyl ((S)-2-((1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexan-2-yl)-1-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoethyl)carbamate |
| SAXA-031 | 828-51-3 | (3r,5r,7r)-adamantane-1-carboxylic acid |
| SAXA-032 | 711-01-3 | methyl (3r,5r,7r)-adamantane-1-carboxylate |
| SAXA-033 | 770-71-8 | ((3r,5r,7r)-adamantan-1-yl)methanol |
| SAXA-034 | 2094-74-8 | (3r,5r,7r)-adamantane-1-carbaldehyde |
| SAXA-035 | - | (R)-2-amino-2-phenylethan-1-ol |
| SAXA-036 | 361441-95-4 | (S)-2-((3S,5S,7S)-adamantan-1-yl)-2-(((R)-2-hydroxy-1-phenylethyl)amino)acetonitrile |
| SAXA-037 | 361441-96-5 | (S)-2-((3S,5S,7S)-adamantan-1-yl)-2-(((R)-2-hydroxy-1-phenylethyl)amino)acetic acid hydrochloride |
| SAXA-038 | 95853-35-3 | (S)-2-((3S,5S,7S)-adamantan-1-yl)-2-aminoacetic acid |
| SAXA-039 | 361441-97-6 | (S)-2-((3S,5S,7S)-adamantan-1-yl)-2-((tert-butoxycarbonyl)amino)acetic acid |
| SAXA-040 | 361442-00-4Available | (S)-2-((tert-butoxycarbonyl)amino)-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-041 | 361440-69-9 | (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide 2,2,2-trifluoroacetate |
OptimisedRoute 3Steps 6 · Total yield /
SAXA-042865999-64-0SAXA-043859202-35-0SAXA-044865999-65-1SAXA-045865999-66-2SAXA-046865999-67-3SAXA-047865999-68-4SAXA-048865999-70-8API · Saxagliptin Hydrate
| Code | CAS No. | Intermediate |
|---|---|---|
| SAXA-042 | 865999-64-0 | (S)-2-amino-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid hydrochloride |
| SAXA-043 | 859202-35-0 | (S)-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-(2,2,2-trifluoroacetamido)acetic acid |
| SAXA-044 | 865999-65-1 | (S)-2-(2,2,2-trifluoroacetamido)-2-((1r,3R,5R,7S)-3-(2,2,2-trifluoroacetoxy)adamantan-1-yl)acetic acid |
| SAXA-045 | 865999-66-2 | (1R,3r,5R,7S)-3-((S)-2-chloro-2-oxo-1-(2,2,2-trifluoroacetamido)ethyl)adamantan-1-yl 2,2,2-trifluoroacetate |
| SAXA-046 | 865999-67-3 | (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrochloride |
| SAXA-047 | 865999-68-4 | (1R,3r,5R,7S)-3-((S)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxo-1-(2,2,2-trifluoroacetamido)ethyl)adamantan-1-yl 2,2,2-trifluoroacetate |
| SAXA-048 | 865999-70-8 | N-((S)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-1-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoethyl)-2,2,2-trifluoroacetamide |
OptimisedRoute 4Steps 10 · Total yield /
SAXA-004178172-26-4SAXA-006709031-38-9SAXA-007361440-67-7SAXA-009361442-01-5SAXA-011709031-43-6SAXA-020709031-29-8SAXA-03895853-35-3SAXA-040361442-00-4SAXA-049709031-39-0SAXA-0501660-04-4SAXA-05116091-98-8API · Saxagliptin Hydrate
| Code | CAS No. | Intermediate |
|---|---|---|
| SAXA-004 | 178172-26-4Available | 1-(tert-butyl) 2-ethyl (S)-2,3-dihydro-1H-pyrrole-1,2-dicarboxylate |
| SAXA-006 | 709031-38-9 | tert-butyl (S)-2-carbamoyl-2,3-dihydro-1H-pyrrole-1-carboxylate |
| SAXA-007 | 361440-67-7Available | tert-butyl (1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexane-2-carboxylate |
| SAXA-009 | 361442-01-5 | tert-butyl ((S)-2-((1S,3S,5S)-3-carbamoyl-2-azabicyclo[3.1.0]hexan-2-yl)-1-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoethyl)carbamate |
| SAXA-011 | 709031-43-6 | tert-butyl ((S)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-1-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)-2-oxoethyl)carbamate |
| SAXA-020 | 709031-29-8 | (S)-2-amino-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-038 | 95853-35-3 | (S)-2-((3S,5S,7S)-adamantan-1-yl)-2-aminoacetic acid |
| SAXA-040 | 361442-00-4Available | (S)-2-((tert-butoxycarbonyl)amino)-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetic acid |
| SAXA-049 | 709031-39-0 | (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carboxamide hydrochloride |
| SAXA-050 | 1660-04-4 | 1-((3r,5r,7r)-adamantan-1-yl)ethanone |
| SAXA-051 | 16091-98-8 | 2-((3r,5r,7r)-adamantan-1-yl)-2-oxoacetic acid |
Frequently asked questions
What are the approved indications of Saxagliptin Hydrate?
Approved indications include: Type 2 diabetes.
When does the Saxagliptin Hydrate patent expire?
No public expiry year is available for Saxagliptin Hydrate yet; this page updates once verified.
How many synthesis routes are recorded for Saxagliptin Hydrate?
4 synthesis routes are recorded; the shortest is 6 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Saxagliptin Hydrate intermediates?
5 intermediate CAS of Saxagliptin Hydrate are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for Saxagliptin Hydrate intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-29