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Pilocarpine Hydrochloride

Tier C — Watch / trade

Pilocarpine Hydrochloride

Alcon Inc
Originator
1951
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type

Targets:mAChRs

Brand:Spersacarpin, PilaSite, Pilocarpina lux, Pilobuc, Pilopine HS, Isopto-<span class="highlightText">pilocarpine</span>, Pilogel, Salagen, Isopto carpine, Pilo, Pilocar

Indications (approved):闭角型青光眼, Ocular hypertension, Open-angle glaucoma, 瞳孔缩小, Sjögren's syndrome, 虹膜炎, 口腔干燥, Glaucoma

Regional status

US
Approved
1974-07-29
EU
No progress
2015-05-01
China
Approved
1981-01-01
Japan
Approved
1967-02-01

Synthetic routes & intermediates5 routes

Originator routes × 0Optimised (non-patent) × 5Process 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 2Steps 7 · Total yield /
(I)115092-6-a636-61-3(II)115092-6-a70681-41-3(III)115092-6-a75-03-6(IV)115092-6-a—(V)115092-6-a—(VI)115092-6-a—(VII)115092-6-a39021-62-0(VIII)115092-6-a—(IX)115092-6-a—API · Pilocarpine Hydrochloride
CodeCAS No.Intermediate
(I)115092-6-a636-61-3(2R)-2-Hydroxysuccinic acid
(II)115092-6-a70681-41-3(R)-2-Hydroxysuccinic acid dimethylester
(III)115092-6-a75-03-6Available1-Iodoethane
(IV)115092-6-a-Diethyl (2S,3R)-2-methyl-3-hydroxysuccinate
(V)115092-6-a-Dimethyl (2S,3R)-2-ethyl-3-[(4-nitrobenzene-1-sulfonyl)oxy]butanedioate
(VI)115092-6-a-Dimethyl (3R)-2-bromo-3-ethylbutanedioate
(VII)115092-6-a39021-62-01-Methyl-1H-imidazole-5-carbaldehyde
(VIII)115092-6-a-Methyl (3S,4S)-4-ethyl-2-(1-methyl-1H-imidazol-5-yl)-5-oxooxolane-3-carboxylate
(IX)115092-6-a-(2S,3R)-2-Ethyl-4-methoxy-3-[(1-methyl-1H-imidazol-5-yl)methyl]-4-oxobutanoic acid
OptimisedRoute 3Steps 4 · Total yield /
(I)115092-7-a123-72-8(II)115092-7-a922-68-9(III)115092-7-a—(IV)115092-7-a—(V)115092-7-a—(VI)115092-7-a—API · Pilocarpine Hydrochloride
CodeCAS No.Intermediate
(I)115092-7-a123-72-81-Butanone
(II)115092-7-a922-68-9Glyoxylic acid methyl ester
(III)115092-7-a-Methyl (2R,3S)-3-formyl-2-hydroxypentanoate
(IV)115092-7-a-(2S,3R)-2-Ethyl-3-hydroxy-4-methoxy-4-oxobutanoic acid
(V)115092-7-a-Diethyl (2S,3R)-2-methyl-3-hydroxysuccinate
(VI)115092-7-a-Dimethyl (2S,3R)-2-ethyl-3-[(4-methylbenzene-1-sulfonyl)oxy]butanedioate
OptimisedRoute 4Steps 4 · Total yield /
(I)115092-8-a636-61-3(IIa)115092-8-a7554-28-1(IIb)115092-8-a83540-97-0(III)115092-8-a75-03-6(IVa)115092-8-a—(IVb)115092-8-a—(Va)115092-8-a—(Vb)115092-8-a—(VIa)115092-8-a—(VIb)115092-8-a—API · Pilocarpine Hydrochloride
CodeCAS No.Intermediate
(I)115092-8-a636-61-3(2R)-2-Hydroxysuccinic acid
(IIa)115092-8-a7554-28-1(R)-Diethyl malate
(IIb)115092-8-a83540-97-0(R)-Diisopropyl 2-hydroxysuccinate
(III)115092-8-a75-03-6Available1-Iodoethane
(IVa)115092-8-a-Diethyl (2S,3R)-2-ethyl-3-hydroxybutanedioate
(IVb)115092-8-a-Dipropan-2-yl (2S,3R)-2-ethyl-3-hydroxybutanedioate
(Va)115092-8-a-Diethyl (2S,3R)-2-ethyl-3-[(4-nitrobenzene-1-sulfonyl)oxy]butanedioate
(Vb)115092-8-a-Dipropan-2-yl (2S,3R)-2-ethyl-3-[(4-nitrobenzene-1-sulfonyl)oxy]butanedioate
(VIa)115092-8-a-Diethyl (3R)-2-bromo-3-ethylbutanedioate
(VIb)115092-8-a-Diisopropyl 2-bromo-3(R)-ethyl-butanedioate
OptimisedRoute 5Steps 6 · Total yield /
(I)115092-10-a—(II)115092-10-a542-78-9(III)115092-10-a—(IV)115092-10-a—(V)115092-10-a—(VI)115092-10-a—(VII)115092-10-a—(VIII)115092-10-a—API · Pilocarpine Hydrochloride
CodeCAS No.Intermediate
(I)115092-10-a-Methyl (2S)-2-hydroxybutanoate
(II)115092-10-a542-78-91,3-Propanedial
(III)115092-10-a-Methyl (2S)-2-ethyl-3-formyl-4-oxobutanoate
(IV)115092-10-a-Methyl (2S)-2-ethyl-4-hydroxy-3-(hydroxymethyl)butanoate
(V)115092-10-a-(3S)-3-Ethyl-4-(hydroxymethyl)oxolan-2-one
(VI)115092-10-a-5-Chloro-1-methyl-1H-imidazole
(VII)115092-10-a-(3S)-3-Ethyl-4-(1-methyl-1H-imidazole-5-carbonyl)oxolan-2-one
(VIII)115092-10-a-(3S)-3-Ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]oxolan-2-one
RouteRoute 1Steps 10 · Total yield 150mg(Pilocarpine Nitrate (API))
Pilocarpine Nitrate-02099776-32-6Pilocarpine Nitrate-021119117-34-9Pilocarpine Nitrate-022144461-05-2Pilocarpine Nitrate-023144461-06-3Pilocarpine Nitrate-0241826-67-1Pilocarpine Nitrate-0251192231-10-9Pilocarpine Nitrate-0261192231-09-6Pilocarpine Nitrate-027144461-10-9Pilocarpine Nitrate-028144461-11-0Pilocarpine Nitrate-01374-89-5Pilocarpine Nitrate-029—Pilocarpine Nitrate-03038993-98-5API · Pilocarpine Hydrochloride
CodeCAS No.Intermediate
Pilocarpine Nitrate-02099776-32-62-(2,2-Dimethoxyethyl)propane-1,3-diol
Pilocarpine Nitrate-021119117-34-92-[(Acetyloxy)methyl]-4,4-dimethoxybutyl acetate
Pilocarpine Nitrate-022144461-05-2(2R)-2-(Hydroxymethyl)-4,4-dimethoxybutyl acetate
Pilocarpine Nitrate-023144461-06-3(2S)-2-Formyl-4,4-dimethoxybutyl acetate
Pilocarpine Nitrate-0241826-67-1Vinylmagnesium bromide
Pilocarpine Nitrate-0251192231-10-9(2S)-2-(2,2-Dimethoxyethyl)pent-4-ene-1,3-diol
Pilocarpine Nitrate-0261192231-09-6(5S)-5-(2,2-Dimethoxyethyl)-4-ethenyl-1,3-dioxan-2-one
Pilocarpine Nitrate-027144461-10-9(3R,4R)-4-(2,2-Dimethoxyethyl)-3-ethenyldihydrofuran-2(3H)-one
Pilocarpine Nitrate-028144461-11-0[(3R,4R)-4-Ethenyl-5-oxotetrahydrofuran-3-yl]acetaldehyde
Pilocarpine Nitrate-01374-89-5Methylamine
Pilocarpine Nitrate-029-(4R)-3-Ethylidene-4-[(2E)-2-(methylimino)ethyl]dihydrofuran-2(3H)-one
Pilocarpine Nitrate-03038993-98-5(3E,4R)-3-Ethylidene-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one

Frequently asked questions

What are the approved indications of Pilocarpine Hydrochloride?

Approved indications include: 闭角型青光眼, Ocular hypertension, Open-angle glaucoma, 瞳孔缩小, Sjögren's syndrome, 虹膜炎, 口腔干燥, Glaucoma.

When does the Pilocarpine Hydrochloride patent expire?

No public expiry year is available for Pilocarpine Hydrochloride yet; this page updates once verified.

How many synthesis routes are recorded for Pilocarpine Hydrochloride?

5 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Pilocarpine Hydrochloride intermediates?

1 intermediate CAS of Pilocarpine Hydrochloride 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 Pilocarpine Hydrochloride 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) · 2026-09-27