ROTIGOTINE Basic Product Information

Product Name	ROTIGOTINE	CAS	99755-59-6
Synonyms	Rotigotine;	Molecular Formula	C19H25NOS
EINECS Number		Molecular Structure
Appearance	Light Yellow Powder
Purity
Supply Ability

ROTIGOTINE Quality documents

ROTIGOTINE Appearance/Package/Shipping/Storage

package

storage condition

Store in cool & dry place,Keep away from strong light and heat

ROTIGOTINE Application

ROTIGOTINE literature

Preparation method of rotigotine

-

, (2021/08/11)

The invention relates to the technical field of medicine preparation, and discloses a preparation method of rotigotine, which comprises the following steps: by taking 5-methoxy-2-tetralone as an initial raw material, reacting with R-alpha-methylbenzylamine, performing debenzylation reduction and S-mandelic acid chiral resolution, then reacting with a propionyl chloride reagent to generate an amide compound, and then reducing by a sodium borohydride reagent to obtain the rotigotine; and finally, reacting with 2-(thiophene-2-yl) 2-nitric acid benzene sulfonic acid ethyl ester to obtain the rotigotine. The preparation process route is as follows: the rotigotine is mild in preparation condition, simple and convenient to operate, relatively high in yield of key intermediates, high in optical purity and easy for industrial large-scale production, and has a very good application prospect.

Synthesis of Pharmaceutically Relevant 2-Aminotetralin and 3-Aminochroman Derivatives via Enzymatic Reductive Amination

Citoler, Joan,Harawa, Vanessa,Marshall, James R.,Bevinakatti, Han,Finnigan, James D.,Charnock, Simon J.,Turner, Nicholas J.

, p. 24456 - 24460 (2021/10/19)

2-Aminotetralin and 3-aminochroman derivatives are key structural motifs present in a wide range of pharmaceutically important molecules. Herein, we report an effective biocatalytic approach towards these molecules through the enantioselective reductive coupling of 2-tetralones and 3-chromanones with a diverse range of primary amine partners. Metagenomic imine reductases (IREDs) were employed as the biocatalysts, obtaining high yields and enantiocomplementary selectivity for >15 examples at preparative scale, including the precursors to Ebalzotan, Robalzotan, Alnespirone and 5-OH-DPAT. We also present a convergent chemo-enzymatic total synthesis of the Parkinson's disease therapy Rotigotine in 63 % overall yield and 92 % ee.

Preparation method for rotigotine

-

, (2019/04/17)

The invention discloses a preparation method for rotigotine. The preparation method includes the following steps: S1. performing an amination reduction reaction on a 5-methoxy-2-tetralone solution, tert-butanesulfinamide, a catalyst, and sodium borohydride to obtain a substance A; S2. performing an alkylation reaction on a solution of the substance A, bromopropane, and a basic catalyst to obtain asubstance B; S3. reacting the substance B with a hydrochloric acid methanol solution to obtain a substance C; S4. performing a reaction on the substance C, 2-(2-bromoethyl)thiophene, potassium carbonate, and N,N-dimethylformamide to obtain a substance D; and S5. reacting acetic acid with hydrogen bromide to obtain the rotigotine. The preparation method is simple in operation, is high in yield, ismild in reaction condition, is green and environmentally friendly, is high in purity of the prepared rotigotine, and is suitable for large-scale industrial production.

Novel Process for Preparation of Rotigotine and Intermediates Thereof

-

, (2019/08/26)

The present invention relates to a novel process for the preparation of Rotigotine of formula (I) and intermediates thereof.

ROTIGOTINE Upstream and downstream

99755-59-6 Upstream product

• 125572-93-2

  rotigotine hydrochloride 

• 40412-06-4

  2-(2-thienyl)ethyl tosylate 

• 101470-23-9

  Desthienyl-Rotigotine 

• 1918-77-0

  Thiophene-2-acetic acid 

• 165950-84-5

  (S)-1,2,3,4-tetrahydro-5-hydroxy-N-propyl-naphthalen-2-ammonium hydrobromide 

• 1222074-06-7

  2-(thiophen-2-yl)ethyl 2-nitrobenzene-1-sulfonate 

• 1222074-05-6

  (S)-2-(N-n-propyl-N-2-(thien-2-yl)ethylamino)-5-methoxytetraline hydrobromide 

• 1229620-82-9

  (S)-6-(propyl(2-(thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-yl acetate hydrochloride 

99755-59-6 Downstream Products

• 125572-93-2

  rotigotine hydrochloride 

• 1229620-82-9

  (S)-6-(propyl(2-(thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-yl acetate hydrochloride 

• 1154425-10-1

  (S)-6-(propyl(2-thiophen-2-ylethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol hydrogen tartrate 

• 1259483-19-6

  (S)-6-(propyl(2-thiophen-2-ylethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol dihydrogen citrate 

• 1259483-21-0

  (S)-6-(propyl(2-thiophen-2-ylethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol orotate 

• 1154425-09-8

  (S)-6-(propyl(2-thiophen-2-ylethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol dihydrogen phosphate 

• 1259483-23-2

  (S)-6-(propyl(2-thiophen-2-ylethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol hydrogen sulphate 

• 1259483-22-1

  (S)-6-(propyl(2-thiophen-2-ylethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol 1-hydroxy-2-naphtoate 

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