tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

Base Information

Chemical Name:tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate
CAS No.:918308-82-4
Molecular Formula:C₃₄H₃₉N₅O₄S
Molecular Weight:613.781
Hs Code.:

tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

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Chemical Property of tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

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Technology Process of tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

There total 4 articles about tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

: 881997-05-3
tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-2-chloro-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

: 918308-82-4
tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

Guidance literature:: Multi-step reaction with 3 steps

1: 815 mg / Na₂CO₃ / Pd(Ph₃P)4 / 1,2-dimethoxy-ethane; H₂O / 23 h / Heating

2: 649 mg / CBr₄; Ph₃P / CH₂Cl₂; tetrahydrofuran / 0.5 h / 0 °C

3: 227 mg / tetrahydrofuran / 64 h / 0 - 20 °C

With carbon tetrabromide; sodium carbonate; triphenylphosphine; tetrakis(triphenylphosphine) palladium⁽⁰⁾; In tetrahydrofuran; 1,2-dimethoxyethane; dichloromethane; water; 1: Suzuki cross-coupling;
DOI:10.1016/j.bmc.2006.08.037

Reference yield:

: 59016-93-2
p-hydroxymethylphenylboronic acid

: 918308-82-4
tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

Guidance literature:: Multi-step reaction with 3 steps

1: 815 mg / Na₂CO₃ / Pd(Ph₃P)4 / 1,2-dimethoxy-ethane; H₂O / 23 h / Heating

2: 649 mg / CBr₄; Ph₃P / CH₂Cl₂; tetrahydrofuran / 0.5 h / 0 °C

3: 227 mg / tetrahydrofuran / 64 h / 0 - 20 °C

With carbon tetrabromide; sodium carbonate; triphenylphosphine; tetrakis(triphenylphosphine) palladium⁽⁰⁾; In tetrahydrofuran; 1,2-dimethoxyethane; dichloromethane; water; 1: Suzuki cross-coupling;
DOI:10.1016/j.bmc.2006.08.037

Reference yield:

: 918309-14-5
tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-2-[4-(hydroxymethyl)phenyl]-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

: 918308-82-4
tert-butyl (2E)-3-(8-{[(4-tert-butyl-1,3-thiazol-2-yl)amino]carbonyl}-4-oxo-2-[4-(pyrrolidin-1-ylmethyl)phenyl]-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylate

Guidance literature:: Multi-step reaction with 2 steps

1: 649 mg / CBr₄; Ph₃P / CH₂Cl₂; tetrahydrofuran / 0.5 h / 0 °C

2: 227 mg / tetrahydrofuran / 64 h / 0 - 20 °C

With carbon tetrabromide; triphenylphosphine; In tetrahydrofuran; dichloromethane;
DOI:10.1016/j.bmc.2006.08.037