Organic synthesis in drug development Flashcards

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1
Q

linear, convergent and parallel sythesis

A

singular reactions designed to make one compound in each reaction vessel

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2
Q

linear, convergent and parallel synthesis are useful for __

A

targeted libraries (lead optimization)

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3
Q

combinatorial chemistry:

A

collection of techniques that allow for the simultaneous generation of large numbers of chemical compounds at the same time using a variety of starting materials

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4
Q

combinatorial chemistry tests

A

a mixture of compounds (high throughput screening)

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5
Q

diversity-oriented synthesis

A

designed to produce as many diverse compounds as possible from a single scaffold

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6
Q

protecting group:

A

inert group intended to mask the reactivity of a particular functional group to prevent it from interfering with the desired reaction

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7
Q

_____ used to make small sets of targeted analogues

A

linear, convergent, parallel synthesis

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8
Q

linear, convergent and parallel synthesis are usually performed in the __ phase

A

solution

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9
Q

linear synthesis:

A

sequential reactions in which product of first reaction is used in the next reaction in a linear fashion

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10
Q

convergent synthesis:

A

approach designed to improve overall yield of final compound by synthesizing fragments before coupling them together in final reaction

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11
Q

parallel synthesis:

A

performing organic reactions (often the same reaction) side by side to generate diverse compounds for SAR

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12
Q

in parallel synthesis, modifications of lead to generate diversity should

A

be made at last possible step

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13
Q

in organic synthesis for SAR, a lead scaffold is used to generate __ optimized analogues

A

less than 100

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14
Q

With organic synthesis for SAR, less than ___ reactions is OK, less than ____ is ideal

A

10/5

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15
Q

combinatorial chemistry:

A

a particular set of building blocks or precursors are used to prepare all possible derivatives of a given compound class

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16
Q

combinatorial chemistry synthesizes compounds ______ and can test ___

A

in a single vessel/ as a mixture

17
Q

combinatorial chemistry: if you have an active mixture:

A

identify active component

18
Q

combinatorial chemistry: if you have an inactive mixture:

A

store for next high througput screening

19
Q

In solid-phase organic synthesis, the starting compound is ______ bound to ______ and sequential reactions are performed to produce ______

A

covalently/ insoluble resin bead/ a library of diverse compounds

20
Q

the ___ and __ used in solid-phase organic synthesis are soluble

A

linker/ reagents

21
Q

reactions can be driven to completion with excess reagents that can be easily removed through washing steps: advantage of _____

A

solid phase organic synthesis

22
Q

Are purification steps necessary at intermediate stages of solid-phase organic synthesis?

A

No

23
Q

Can individual beads be separated at the end of solid-phase organic synthesis to give individual products?

A

Yes

24
Q

Can solid-phase organic synthesis be automated?

A

Yes

25
Q

for SPOS, ______ and ______ must be inert to reaction conditions

A

resin bead/ linker

26
Q

the linker in SPOS must be ____ through a _____ such as _______

A

easily cleaved/ direct mechanism/ (acid/base)

27
Q

ideally, in SPOS, _____ should be cleaved through the same mechanism as ____

A

protecting groups/ linkers