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Flashcards in Organic synthesis in drug development Deck (27):
1

linear, convergent and parallel sythesis

singular reactions designed to make one compound in each reaction vessel

2

linear, convergent and parallel synthesis are useful for __

targeted libraries (lead optimization)

3

combinatorial chemistry:

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

4

combinatorial chemistry tests

a mixture of compounds (high throughput screening)

5

diversity-oriented synthesis

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

6

protecting group:

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

7

_____ used to make small sets of targeted analogues

linear, convergent, parallel synthesis

8

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

solution

9

linear synthesis:

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

10

convergent synthesis:

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

11

parallel synthesis:

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

12

in parallel synthesis, modifications of lead to generate diversity should

be made at last possible step

13

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

less than 100

14

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

10/5

15

combinatorial chemistry:

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

16

combinatorial chemistry synthesizes compounds ______ and can test ___

in a single vessel/ as a mixture

17

combinatorial chemistry: if you have an active mixture:

identify active component

18

combinatorial chemistry: if you have an inactive mixture:

store for next high througput screening

19

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

covalently/ insoluble resin bead/ a library of diverse compounds

20

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

linker/ reagents

21

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

solid phase organic synthesis

22

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

No

23

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

Yes

24

Can solid-phase organic synthesis be automated?

Yes

25

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

resin bead/ linker

26

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

easily cleaved/ direct mechanism/ (acid/base)

27

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

protecting groups/ linkers