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Lisaftoclax
Tier C — Watch / tradeLisaftoclax
-
Originator
2025
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：BCL2
Indications (approved)：Chronic lymphocytic leukaemia
Regional status
US
Phase III
2023-12-20
EU
Phase III
2023-12-20
China
Approved
2025-07-08
Japan
-
Synthetic routes & intermediates7 routes
Originator routes × 0Optimised (non-patent) × 7Process 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.
OptimisedRoute 1Steps 10 · Total yield /
(I)992511-1-a,(I)992511-1-d1191-95-3(II)992511-1-a1439-36-7(III)992511-1-a67223-98-7(IX)992511-1-a616-38-6(V)992511-1-a,(V)992511-1-d221342-48-9(VI)992511-1-a221342-47-8(VII)992511-1-a221342-49-0(VIII)992511-1-a,(VIII)992511-1-d74064-35-0(IV)992511-1-a108-59-8(X)992511-1-a2180923-60-6(XI)992511-1-a2180923-61-7(XII)992511-1-a,(XII)992511-1-d1679-18-1(XIII)992511-1-a2180923-62-8(XIV)992511-1-a2180923-63-9(XV)992511-1-a,(XV)992511-1-b2180923-64-0API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)992511-1-a,(I)992511-1-d | 1191-95-3Available | Cyclobutanone |
| (II)992511-1-a | 1439-36-7 | 1-(Triphenylphosphoranylidene)-2-propanone |
| (III)992511-1-a | 67223-98-7 | 1-Cyclobutylidenepropan-2-one |
| (IX)992511-1-a | 616-38-6 | Carbonic acid dimethyl diester |
| (V)992511-1-a,(V)992511-1-d | 221342-48-9 | Spiro[3.5]nonane-6,8-dione |
| (VI)992511-1-a | 221342-47-8 | 8-(2-Methylpropoxy)spiro[3.5]non-7-en-6-one |
| (VII)992511-1-a | 221342-49-0 | Spiro[3.5]non-7-en-6-one |
| (VIII)992511-1-a,(VIII)992511-1-d | 74064-35-0 | Spiro[3.5]nonan-6-one |
| (IV)992511-1-a | 108-59-8Available | 1,3-Dimethyl propanedioate |
| (X)992511-1-a | 2180923-60-6 | Methyl 6-oxospiro[3.5]nonane-7-carboxylate |
| (XI)992511-1-a | 2180923-61-7 | Methyl 6-(((trifluoromethyl)sulfonyl)oxy) spiro[3.5]non-6-ene-7-carboxylate |
| (XII)992511-1-a,(XII)992511-1-d | 1679-18-1Available | (4-Chlorophenyl)boranediol |
| (XIII)992511-1-a | 2180923-62-8 | Methyl 6-(4-chlorophenyl)spiro[3.5]non-6-ene-7-carboxylate |
| (XIV)992511-1-a | 2180923-63-9 | [6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methanol |
| (XV)992511-1-a,(XV)992511-1-b | 2180923-64-0 | 7-(Chloromethyl)-6-(4-chlorophenyl)spiro[3.5]non-6-ene |
OptimisedRoute 2Steps 3 · Total yield /
(XIX)992511-1-b,(XIX)992511-1-g1628174-84-4(XV)992511-1-a,(XV)992511-1-b2180923-64-0(XVI)992511-1-b,(XVI)992511-1-c2180923-73-1(XVII)992511-1-b2180923-74-2(XVIII)992511-1-b,(XVIII)992511-1-e,(XVIII)992511-1-f2180923-75-3API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIX)992511-1-b,(XIX)992511-1-g | 1628174-84-4 | 3-Nitro-4-[[(2S)-1,4-dioxan-2-yl]methylamino]benzenesulfonamide |
| (XV)992511-1-a,(XV)992511-1-b | 2180923-64-0 | 7-(Chloromethyl)-6-(4-chlorophenyl)spiro[3.5]non-6-ene |
| (XVI)992511-1-b,(XVI)992511-1-c | 2180923-73-1 | Ethyl 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(piperazin-1 -yl)benzoate |
| (XVII)992511-1-b | 2180923-74-2 | Ethyl 4-(4-[[6-(4-chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazin-1-yl)-2-[(1H-pyrrolo[2,3-b]pyridin-5-yl)oxy]benzoate |
| (XVIII)992511-1-b,(XVIII)992511-1-e,(XVIII)992511-1-f | 2180923-75-3 | 4-(4-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazin-1-yl)-2-[(1H-pyrrolo[2,3-b]pyridin-5-yl)oxy]benzoic acid |
OptimisedRoute 3Steps 3 · Total yield /
(XVI)992511-1-b,(XVI)992511-1-c2180923-73-1(XX)992511-1-c108928-00-3(XXI)992511-1-c685514-01-6(XXII)992511-1-c2169699-38-9(XXIII)992511-1-c,(XXIII)992511-1-d57260-71-6(XXIV)992511-1-c2180923-72-0API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (XVI)992511-1-b,(XVI)992511-1-c | 2180923-73-1 | Ethyl 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(piperazin-1 -yl)benzoate |
| (XX)992511-1-c | 108928-00-3 | Ethyl 2,4-difluorobenzoate |
| (XXI)992511-1-c | 685514-01-6Available | 1-(Triisopropylsilyl)-1H-pyrrolo[2,3-b]pyridin-5-ol |
| (XXII)992511-1-c | 2169699-38-9 | Ethyl 2-((1H-pyrrolo[2,3-b]pyridin-5- yl)oxy)-4-fluorobenzoate |
| (XXIII)992511-1-c,(XXIII)992511-1-d | 57260-71-6Available | 1-(1,1-Dimethylethoxycarbonyl)piperazine |
| (XXIV)992511-1-c | 2180923-72-0 | tert-Butyl 4-[4-(ethoxycarbonyl)-3-[(1H-pyrrolo[2,3-b]pyridin-5-yl)oxy]phenyl]piperazine-1-carboxylate |
OptimisedRoute 4Steps 8 · Total yield /
(I)992511-1-a,(I)992511-1-d1191-95-3(V)992511-1-a,(V)992511-1-d221342-48-9(VIII)992511-1-a,(VIII)992511-1-d74064-35-0(XII)992511-1-a,(XII)992511-1-d1679-18-1(XXIII)992511-1-c,(XXIII)992511-1-d57260-71-6(XXIX)992511-1-d2757573-96-7(XXV)992511-1-d867-13-0(XXVI)992511-1-d—(XXVII)992511-1-d105-50-0(XXVIII)992511-1-d68-12-2(XXX)992511-1-d2757573-97-8(XXXI)992511-1-d2757573-98-9(XXXII)992511-1-d2757574-00-6(XXXIII)992511-1-d,(XXXIII)992511-1-e,(XXXIII)992511-1-f2757573-99-0API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)992511-1-a,(I)992511-1-d | 1191-95-3Available | Cyclobutanone |
| (V)992511-1-a,(V)992511-1-d | 221342-48-9 | Spiro[3.5]nonane-6,8-dione |
| (VIII)992511-1-a,(VIII)992511-1-d | 74064-35-0 | Spiro[3.5]nonan-6-one |
| (XII)992511-1-a,(XII)992511-1-d | 1679-18-1Available | (4-Chlorophenyl)boranediol |
| (XXIII)992511-1-c,(XXIII)992511-1-d | 57260-71-6Available | 1-(1,1-Dimethylethoxycarbonyl)piperazine |
| (XXIX)992511-1-d | 2757573-96-7 | 6-Chlorospiro[3.5]non-6-ene-7-carbaldehyde |
| (XXV)992511-1-d | 867-13-0Available | (Diethoxyphosphinyl)acetic acid ethyl ester |
| (XXVI)992511-1-d | - | Ethyl cyclobutylideneacetate |
| (XXVII)992511-1-d | 105-50-0 | 1,3-Acetonedicarboxylic acid diethyl ester |
| (XXVIII)992511-1-d | 68-12-2 | Formyldimethylamine |
| (XXX)992511-1-d | 2757573-97-8 | 6-(4-Chlorophenyl)spiro[3.5]non-6-ene-7-carbaldehyde |
| (XXXI)992511-1-d | 2757573-98-9 | N-Boc-1-[[8-(4-chlorophenyl)spiro[3.5]non-7-en-7-yl]methyl]piperazine |
| (XXXII)992511-1-d | 2757574-00-6 | 1-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazine dihydrogen chloride |
| (XXXIII)992511-1-d,(XXXIII)992511-1-e,(XXXIII)992511-1-f | 2757573-99-0 | 1-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazine |
OptimisedRoute 5Steps 4 · Total yield /
(XVIII)992511-1-b,(XVIII)992511-1-e,(XVIII)992511-1-f2180923-75-3(XXXIII)992511-1-d,(XXXIII)992511-1-e,(XXXIII)992511-1-f2757573-99-0(XXXIV)992511-1-e2757574-02-8(XXXV)992511-1-e2757574-03-9(XXXVI)992511-1-e112704-79-7(XXXVII)992511-1-e2757574-01-7(XXXVIII)992511-1-e98549-88-3API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (XVIII)992511-1-b,(XVIII)992511-1-e,(XVIII)992511-1-f | 2180923-75-3 | 4-(4-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazin-1-yl)-2-[(1H-pyrrolo[2,3-b]pyridin-5-yl)oxy]benzoic acid |
| (XXXIII)992511-1-d,(XXXIII)992511-1-e,(XXXIII)992511-1-f | 2757573-99-0 | 1-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazine |
| (XXXIV)992511-1-e | 2757574-02-8 | 1,1-Dimethylpropyl 4-bromo-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoate |
| (XXXV)992511-1-e | 2757574-03-9 | 2-Methylbutan-2-yl 4-(4-[[6-(4-chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazin-1-yl)-2-[(1H-pyrrolo[2,3-b]pyridin-5-yl)oxy]benzoate |
| (XXXVI)992511-1-e | 112704-79-7 | 4-Bromo-2-fluorobenzene carboxylic acid |
| (XXXVII)992511-1-e | 2757574-01-7 | 1,1-Dimethylpropyl 4-bromo-2-fluoro-benzoate |
| (XXXVIII)992511-1-e | 98549-88-3Available | 1H-Pyrrolo[2,3-b]pyridin-5-ol |
OptimisedRoute 6Steps 1 · Total yield /
(XVIII)992511-1-b,(XVIII)992511-1-e,(XVIII)992511-1-f2180923-75-3(XXXIII)992511-1-d,(XXXIII)992511-1-e,(XXXIII)992511-1-f2757573-99-0(XXXIX)992511-1-f2131743-82-1API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (XVIII)992511-1-b,(XVIII)992511-1-e,(XVIII)992511-1-f | 2180923-75-3 | 4-(4-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazin-1-yl)-2-[(1H-pyrrolo[2,3-b]pyridin-5-yl)oxy]benzoic acid |
| (XXXIII)992511-1-d,(XXXIII)992511-1-e,(XXXIII)992511-1-f | 2757573-99-0 | 1-[[6-(4-Chlorophenyl)spiro[3.5]non-6-en-7-yl]methyl]piperazine |
| (XXXIX)992511-1-f | 2131743-82-1 | 2-[(7-Azaindole-5-yl)oxy]-4-bromobenzoic acid |
OptimisedRoute 7Steps 1 · Total yield /
(XIX)992511-1-b,(XIX)992511-1-g1628174-84-4(XL)992511-1-g1523541-96-9(XLI)992511-1-g97-09-6API · Lisaftoclax
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIX)992511-1-b,(XIX)992511-1-g | 1628174-84-4 | 3-Nitro-4-[[(2S)-1,4-dioxan-2-yl]methylamino]benzenesulfonamide |
| (XL)992511-1-g | 1523541-96-9 | (S)-2-Aminomethyl-1,4-dioxane hydrochlorid |
| (XLI)992511-1-g | 97-09-6 | 3-Nitro-4-chlorobenzensulfonyl amine |
Frequently asked questions
What are the approved indications of Lisaftoclax?
Approved indications include: Chronic lymphocytic leukaemia.
When does the Lisaftoclax patent expire?
No public expiry year is available for Lisaftoclax yet; this page updates once verified.
How many synthesis routes are recorded for Lisaftoclax?
7 synthesis routes are recorded; the shortest is 1 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Lisaftoclax intermediates?
7 intermediate CAS of Lisaftoclax 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 Lisaftoclax 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) · 2026-10-22